| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| Ab170524-100μg |
100μg |
现货  |
| |
| Ab170524-1mg |
1mg |
现货 |
| |
| Ab170524-5mg |
5mg |
现货 |
| |
| Ab170524-10mg |
10mg |
期货 |
|
| 产品名称 | Margetuximab (anti-HER2), erb-b2 受体酪氨酸激酶 2 抗体 |
|---|---|
| 别名 | 玛格妥昔单抗 | Margetuximab（抗 HER2） |
| 英文别名 | Verb b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived oncogene homolog antibody | C erb B2/neu protein antibody | CD340 antibody | CD340 antigen antibody | Cerb B2/neu protein antibody | CerbB2 antibody | Erb b2 receptor tyr |
| 规格或纯度 | 无载体, 重组, ExactAb™, 低内毒素, 无叠氮钠, 已验证, 无动物源, ≥95%(SDS-PAGE&SEC-HPLC), 见COA |
| 宿主种属 | 人(Human) |
| 特异性 | ErbB2 |
| 应用 | ELISA,Functional Assay,Flow cytometry,Kinetics (BLI),Kinetics (SPR) |
| 种属反应性 | 人(Human),小鼠(Mouse) |
| 偶联 | Unconjugated |
| 作用类型 | 抑制剂 |
| 作用机制 | erb-b2 受体酪氨酸激酶 2 抗体 |
| 抗体类型 | Primary antibody |
|---|---|
| 克隆类型 | 重组抗体 |
| Format | Whole IgG |
| 亚型 | Human IgG1 |
| 轻链亚型 | kappa |
| SDS-PAGE | 26.6 kDa (Light Chain) & 51.9 kDa (Heavy Chain), under reducing conditions; 179.3 kDa, under non-reducing conditions. |
| 纯化方法 | Protein A purified |
| 纯度 | >95% |
| 来源 | CHO supernatant |
| 物理外观 | Liquid |
| 储存缓冲液 | Supplied as a 0.22 μm filtered solution in 100mM Pro-Ac, 20mM Arg, pH 5.0 |
| 防腐剂 | No |
| 浓度 | 见COA |
| 储存温度 | -80℃储存,避免反复冻融 |
| 运输条件 | 超低温冰袋运输 |
| 稳定性与储存 | 在 -80℃ 下保存 24 个月。收货后建议分装。避免冷冻/解冻循环。 |
| CAS编号和信息 | 1350624-75-7 |
| 分子类型 | 抗体 |
Margetuximab (anti-HER2) (Ab170524) - Flow Cytometry
Flow Cytometry analysis of MCF-7 cells labelling HER2 (red) with Margetuximab (anti-HER2) (Ab170524). Goat Anti-Human IgG (PE) (Ab175838) at a dilution of 1/1000 was used as the secondary antibody. Blue - Isotype control, human IgG (Ab170213). Black - Unlabelled control, cells without incubation with primary antibody.
Margetuximab (anti-HER2) (Ab170524) - SEC
The purity of Margetuximab (anti-HER2) (Ab170524) is more than 95% verified by HPLC.
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 日期 | 货号 |
|---|---|---|---|
 ZJ24F0911489 |
分析证书 | 24-09-29 | Ab170524 |
| ZJ24F0911488 |
分析证书 | 24-09-29 | Ab170524 |
| ZJ23F1001271 |
分析证书 | 23-10-13 | Ab170524 |
| ZJ23F1001272 |
分析证书 | 23-10-13 | Ab170524 |
¥669.90
¥669.90
¥669.90
¥193.90
¥489.90
¥479.90
| 1. Catenacci DV, Rosales M, Chung HC, H Yoon H, Shen L, Moehler M, Kang YK. (2020) MAHOGANY: margetuximab combination in HER2+ unresectable/metastatic gastric/gastroesophageal junction adenocarcinoma.. Future Oncol, [PMID:33263418] [10.2217/fon-2020-1007] |
| 2. Dumas J, Hatoum-Mokdad H, Sibley RN, Smith RA, Scott WJ, Khire U, Lee W, Wood J, Wolanin D, Cooley J, Bankston D, Redman AM, Schoenleber R, Caringal Y, Gunn D, Romero R, Osterhout M, Paulsen H, Housley TJ, Wilhelm SM, Pirro J, Chien DS, Ranges GE, Shrikhande A, Muzsi A, Bortolon E, Wakefield J, Gianpaolo Ostravage C, Bhargava A, Chau T.. (2002) Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.. Bioorg Med Chem Lett, 12 (12): (1559-1562). [PMID:12039561] [10.1016/s0960-894x(02)00238-x] |
| 3. Rewcastle GW, Murray DK, Elliott WL, Fry DW, Howard CT, Nelson JM, Roberts BJ, Vincent PW, Showalter HD, Winters RT, Denny WA.. (1998) Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.. J Med Chem, 41 (5): (742-751). [PMID:9513602] [10.1021/jm970641d] |
| 4. Smaill JB, Palmer BD, Rewcastle GW, Denny WA, McNamara DJ, Dobrusin EM, Bridges AJ, Zhou H, Showalter HD, Winters RT, Leopold WR, Fry DW, Nelson JM, Slintak V, Elliot WL, Roberts BJ, Vincent PW, Patmore SJ.. (1999) Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.. J Med Chem, 42 (10): (1803-1815). [PMID:10346932] [10.1021/jm9806603] |
| 5. Berezov A, Zhang HT, Greene MI, Murali R.. (2001) Disabling erbB receptors with rationally designed exocyclic mimetics of antibodies: structure-function analysis.. J Med Chem, 44 (16): (2565-2574). [PMID:11472210] [10.1021/jm000527m] |
| 6. Kim KS, Kimball SD, Misra RN, Rawlins DB, Hunt JT, Xiao HY, Lu S, Qian L, Han WC, Shan W, Mitt T, Cai ZW, Poss MA, Zhu H, Sack JS, Tokarski JS, Chang CY, Pavletich N, Kamath A, Humphreys WG, Marathe P, Bursuker I, Kellar KA, Roongta U, Batorsky R, Mulheron JG, Bol D, Fairchild CR, Lee FY, Webster KR.. (2002) Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.. J Med Chem, 45 (18): (3905-3927). [PMID:12190313] [10.1021/jm0201520] |
| 7. Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S et al.. (2012) 7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.. J Med Chem, 55 (1): (403-13). [PMID:22136433] |
| 8. Aertgeerts K, Skene R, Yano J, Sang BC, Zou H, Snell G, Jennings A, Iwamoto K, Habuka N, Hirokawa A et al.. (2011) Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.. J Biol Chem, 286 (21): (18756-65). [PMID:21454582] |
| 9. Cho HS, Mason K, Ramyar KX, Stanley AM, Gabelli SB, Denney DW, Leahy DJ. (2003) Structure of the extracellular region of HER2 alone and in complex with the Herceptin Fab.. Nature, 421 (6924): (756-60). [PMID:12610629] |
| 10. Rabindran SK, Discafani CM, Rosfjord EC, Baxter M, Floyd MB, Golas J, Hallett WA, Johnson BD, Nilakantan R, Overbeek E et al.. (2004) Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.. Cancer Res, 64 (11): (3958-65). [PMID:15173008] |
| 11. Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM et al.. (2004) Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.. J Med Chem, 47 (27): (6658-61). [PMID:15615512] |
| 12. Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, Blättler WA, Lambert JM, Chari RV, Lutz RJ et al.. (2008) Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate.. Cancer Res, 68 (22): (9280-90). [PMID:19010901] |
| 13. Traxler P, Allegrini PR, Brandt R, Brueggen J, Cozens R, Fabbro D, Grosios K, Lane HA, McSheehy P, Mestan J et al.. (2004) AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.. Cancer Res, 64 (14): (4931-41). [PMID:15256466] |
| 14. Solca FF, Baum A, Langkopf E, Dahmann G, Heider KH, Himmelsbach F, van Meel JC. (2004) Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives.. J Pharmacol Exp Ther, 311 (2): (502-9). [PMID:15199094] |
| 15. Barlaam B, Anderton J, Ballard P, Bradbury RH, Hennequin LF, Hickinson DM, Kettle JG, Kirk G, Klinowska T, Lambert-van der Brempt C et al.. (2013) Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.. ACS Med Chem Lett, 4 (8): (742-6). [PMID:24900741] |
| 16. Ballou LM, Selinger ES, Choi JY, Drueckhammer DG, Lin RZ. (2007) Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.. J Biol Chem, 282 (33): (24463-70). [PMID:17562705] |
| 17. Klutchko SR, Zhou H, Winters RT, Tran TP, Bridges AJ, Althaus IW, Amato DM, Elliott WL, Ellis PA, Meade MA et al.. (2006) Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.. J Med Chem, 49 (4): (1475-85). [PMID:16480284] |
| 18. Zhang P, Hu HR, Huang ZH, Lei JY, Chu Y, Ye DY. (2012) Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.. Bioorg Med Chem Lett, 22 (23): (7232-6). [PMID:23099099] |
| 19. Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ et al.. (2006) Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.. J Med Chem, 49 (12): (3563-80). [PMID:16759099] |
| 20. Aston NM, Bamborough P, Buckton JB, Edwards CD, Holmes DS, Jones KL, Patel VK, Smee PA, Somers DO, Vitulli G et al.. (2009) p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.. J Med Chem, 52 (20): (6257-69). [PMID:19772287] |
| 21. Nam HJ, Kim HP, Yoon YK, Hur HS, Song SH, Kim MS, Lee GS, Han SW, Im SA, Kim TY et al.. (2011) Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer.. Cancer Lett, 302 (2): (155-65). [PMID:21306821] |
| 22. Conway JG, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM et al.. (2005) Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.. Proc Natl Acad Sci USA, 102 (44): (16078-83). [PMID:16249345] |
| 23. Misra RN, Xiao HY, Kim KS, Lu S, Han WC, Barbosa SA, Hunt JT, Rawlins DB, Shan W, Ahmed SZ et al.. (2004) N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.. J Med Chem, 47 (7): (1719-28). [PMID:15027863] |
| 24. Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, Padera RF, Shapiro GI, Baum A, Himmelsbach F et al.. (2008) BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.. Oncogene, 27 (34): (4702-11). [PMID:18408761] |
| 25. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C. (2009) Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).. J Med Chem, 52 (20): (6433-46). [PMID:19788238] |
| 26. McDonagh CF, Huhalov A, Harms BD, Adams S, Paragas V, Oyama S, Zhang B, Luus L, Overland R, Nguyen S et al.. (2012) Antitumor activity of a novel bispecific antibody that targets the ErbB2/ErbB3 oncogenic unit and inhibits heregulin-induced activation of ErbB3.. Mol Cancer Ther, 11 (3): (582-93). [PMID:22248472] |
| 27. Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT, Brown JR et al.. (2016) Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.. N Engl J Med, 374 (4): (323-32). [PMID:26641137] |
| 28. Kim KH, Maderna A, Schnute ME, Hegen M, Mohan S, Miyashiro J, Lin L, Li E, Keegan S, Lussier J et al.. (2011) Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.. Bioorg Med Chem Lett, 21 (21): (6258-63). [PMID:21958547] |
| 29. Hobson AD, Harris CM, van der Kam EL, Turner SC, Abibi A, Aguirre AL, Bousquet P, Kebede T, Konopacki DB, Gintant G et al.. (2015) Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.. J Med Chem, 58 (23): (9154-70). [PMID:26509640] |
| 30. Li X, Yang C, Wan H, Zhang G, Feng J, Zhang L, Chen X, Zhong D, Lou L, Tao W et al.. (2017) Discovery and development of pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer.. Eur J Pharm Sci, 110 (51-61). [PMID:28115222] |
| 31. Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M et al.. (2015) Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.. J Med Chem, 58 (21): (8373-86). [PMID:26505898] |
| 32. Xie H, Lin L, Tong L, Jiang Y, Zheng M, Chen Z, Jiang X, Zhang X, Ren X, Qu W et al.. (2011) AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo.. PLoS ONE, 6 (7): (e21487). [PMID:21789172] |
| 33. Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y et al.. (2015) Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).. J Med Chem, 58 (20): (8182-99). [PMID:26431428] |
| 34. Qi B, Yang Y, Gong G, He H, Yue X, Xu X, Hu Y, Li J, Chen T, Wan X et al.. (2019) Discovery of N1-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)-N3-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)urea as a multi-tyrosine kinase inhibitor for drug-sensitive and drug-resistant cancers treatment.. Eur J Med Chem, 163 (10-27). [PMID:30503936] |
| 35. Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G et al.. (2020) Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.. J Med Chem, 63 (10): (5102-5118). [PMID:32083858] |
| 36. Kulukian A, Lee P, Taylor J, Rosler R, de Vries P, Watson D, Forero-Torres A, Peterson S. (2020) Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models.. Mol Cancer Ther, 19 (4): (976-987). [PMID:32241871] |
| 37. Pietilä M, Sahgal P, Peuhu E, Jäntti NZ, Paatero I, Närvä E, Al-Akhrass H, Lilja J, Georgiadou M, Andersen OM, Padzik A, Sihto H, Joensuu H, Blomqvist M, Saarinen I, Boström PJ, Taimen P, Ivaska J. SORLA regulates endosomal trafficking and oncogenic fitness of HER2.. Nat Commun, [PMID:31138794] |
| 38. Qing-Shan Li,Xian-Hai Lv,Yan-Bin Zhang,Jing-Jun Dong,Wen-Ping Zhou,Yang Yang,Hai-Liang Zhu. (2012-10-03) Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents.. Bioorganic & medicinal chemistry letters, 22 ((21)): (6596-6601). [PMID:23025996] |
| 39. Ajit Dhananjay Jagtap,Pei-Teh Chang,Jia-Rong Liu,Hsiao-Chun Wang,Nagendra B Kondekar,Li-Jiuan Shen,Hsiang-Wen Tseng,Grace Shiahuy Chen,Ji-Wang Chern. (2014-08-05) Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia.. European journal of medicinal chemistry, 85 (268-288). [PMID:25089810] |
| 40. Emily J Hanan,Charles Eigenbrot,Marian C Bryan,Daniel J Burdick,Bryan K Chan,Yuan Chen,Jennafer Dotson,Robert A Heald,Philip S Jackson,Hank La,Michael D Lainchbury,Shiva Malek,Hans E Purkey,Gabriele Schaefer,Stephen Schmidt,Eileen M Seward,Steve Sideris,Christine Tam,Shumei Wang,Siew Kuen Yeap,Ivana Yen,Jianping Yin,Christine Yu,Inna Zilberleyb,Timothy P Heffron. (2014-11-11) Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.. Journal of medicinal chemistry, 57 ((23)): (10176-10191). [PMID:25383627] |
| 41. Xiaoqing Wu,Mingdong Li,Yang Qu,Wenhua Tang,Youguang Zheng,Jiqin Lian,Min Ji,Liang Xu. (2010-05-15) Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.. Bioorganic & medicinal chemistry, 18 ((11)): (3812-3822). [PMID:20466555] |
| 42. Bing Yu,Li-da Tang,Yi-Liang Li,Shu-Hui Song,Xiao-Liang Ji,Mu-Sen Lin,Chun-Fu Wu. (2011-12-16) Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.. Bioorganic & medicinal chemistry letters, 22 ((1)): (110-114). [PMID:22169262] |
| 43. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Rucklin G.. (2004) Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.. Bioorg Med Chem Lett, 14 (13): (3595-3599). [PMID:15177482] [10.1016/j.bmcl.2004.03.106] |
| 44. Hennequin LF, Stokes ES, Thomas AP, Johnstone C, Plé PA, Ogilvie DJ, Dukes M, Wedge SR, Kendrew J, Curwen JO.. (2002) Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.. J Med Chem, 45 (6): (1300-1312). [PMID:11881999] [10.1021/jm011022e] |
| 45. Borzilleri RM, Zheng X, Qian L, Ellis C, Cai ZW, Wautlet BS, Mortillo S, Jeyaseelan R, Kukral DW, Fura A, Kamath A, Vyas V, Tokarski JS, Barrish JC, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS.. (2005) Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.. J Med Chem, 48 (12): (3991-4008). [PMID:15943473] [10.1021/jm0501275] |
| 46. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Neumann U, Rucklin G.. (2006) Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.. Bioorg Med Chem Lett, 16 (2): (262-266). [PMID:16249085] [10.1016/j.bmcl.2005.10.015] |
| 47. Borzilleri RM, Bhide RS, Barrish JC, D'Arienzo CJ, Derbin GM, Fargnoli J, Hunt JT, Jeyaseelan R, Kamath A, Kukral DW, Marathe P, Mortillo S, Qian L, Tokarski JS, Wautlet BS, Zheng X, Lombardo LJ.. (2006) Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.. J Med Chem, 49 (13): (3766-3769). [PMID:16789733] [10.1021/jm060347y] |
| 48. Cheng ZY, Li WJ, He F, Zhou JM, Zhu XF.. (2007) Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase.. Bioorg Med Chem, 15 (3): (1533-1538). [PMID:17174554] [10.1016/j.bmc.2006.09.041] |
| 49. McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, Maheswaran S, Njauw CN, Tsao H, Drew L, Hanke JH, Ma XJ, Erlander MG, Gray NS, Haber DA, Settleman J.. (2007) Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.. Proc Natl Acad Sci U S A, 104 (50): (19936-19941). [PMID:18077425] [10.1073/pnas.0707498104] |
| 50. Hubbard RD, Bamaung NY, Fidanze SD, Erickson SA, Palazzo F, Wilsbacher JL, Zhang Q, Tucker LA, Hu X, Kovar P, Osterling DJ, Johnson EF, Bouska J, Wang J, Davidsen SK, Bell RL, Sheppard GS.. (2009) Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.. Bioorg Med Chem Lett, 19 (6): (1718-1721). [PMID:19217287] [10.1016/j.bmcl.2009.01.086] |
| 51. Hur W, Velentza A, Kim S, Flatauer L, Jiang X, Valente D, Mason DE, Suzuki M, Larson B, Zhang J, Zagorska A, Didonato M, Nagle A, Warmuth M, Balk SP, Peters EC, Gray NS.. (2008) Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.. Bioorg Med Chem Lett, 18 (22): (5916-5919). [PMID:18667312] [10.1016/j.bmcl.2008.07.062] |
| 52. Taldone T, Sun W, Chiosis G.. (2009) Discovery and development of heat shock protein 90 inhibitors.. Bioorg Med Chem, 17 (6): (2225-2235). [PMID:19017562] [10.1016/j.bmc.2008.10.087] |
| 53. Li R, Pourpak A, Morris SW.. (2009) Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.. J Med Chem, 52 (16): (4981-5004). [PMID:19610618] [10.1021/jm9002395] |
| 54. Cha MY, Lee KO, Kim JW, Lee CG, Song JY, Kim YH, Lee GS, Park SB, Kim MS.. (2009) Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.. J Med Chem, 52 (21): (6880-6888). [PMID:19888761] [10.1021/jm901146p] |
| 55. Li J, Kaoud TS, Laroche C, Dalby KN, Kerwin SM.. (2009) Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles.. Bioorg Med Chem Lett, 19 (22): (6293-6297). [PMID:19822424] [10.1016/j.bmcl.2009.09.094] |
| 56. Mahboobi S, Sellmer A, Winkler M, Eichhorn E, Pongratz H, Ciossek T, Baer T, Maier T, Beckers T.. (2010) Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.. J Med Chem, 53 (24): (8546-8555). [PMID:21080629] [10.1021/jm100665z] |
| 57. Ishikawa T, Seto M, Banno H, Kawakita Y, Oorui M, Taniguchi T, Ohta Y, Tamura T, Nakayama A, Miki H, Kamiguchi H, Tanaka T, Habuka N, Sogabe S, Yano J, Aertgeerts K, Kamiyama K.. (2011) Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.. J Med Chem, 54 (23): (8030-8050). [PMID:22003817] [10.1021/jm2008634] |
| 58. Suzuki N, Shiota T, Watanabe F, Haga N, Murashi T, Ohara T, Matsuo K, Omori N, Yari H, Dohi K, Inoue M, Iguchi M, Sentou J, Wada T.. (2012) Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.. Bioorg Med Chem Lett, 22 (1): (456-460). [PMID:22101132] [10.1016/j.bmcl.2011.10.103] |
| 59. Bijian K, Zhang Z, Xu B, Jie S, Chen B, Wan S, Wu J, Jiang T, Alaoui-Jamali MA.. (2012) Synthesis and biological activity of novel organoselenium derivatives targeting multiple kinases and capable of inhibiting cancer progression to metastases.. Eur J Med Chem, 48 (143-152). [PMID:22204902] [10.1016/j.ejmech.2011.12.006] |
| 60. Turrado C, Puig T, García-Cárceles J, Artola M, Benhamú B, Ortega-Gutiérrez S, Relat J, Oliveras G, Blancafort A, Haro D, Marrero PF, Colomer R, López-Rodríguez ML.. (2012) New synthetic inhibitors of fatty acid synthase with anticancer activity.. J Med Chem, 55 (11): (5013-5023). [PMID:22559865] [10.1021/jm2016045] |
| 61. Zhang P, Hu HR, Bian SH, Huang ZH, Chu Y, Ye DY.. (2013) Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β).. Eur J Med Chem, 61 (95-103). [PMID:23047001] [10.1016/j.ejmech.2012.09.021] |
| 62. Yang LL, Li GB, Ma S, Zou C, Zhou S, Sun QZ, Cheng C, Chen X, Wang LJ, Feng S, Li LL, Yang SY.. (2013) Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.. J Med Chem, 56 (4): (1641-1655). [PMID:23362959] [10.1021/jm301537p] |
| 63. Brown A, Shi Q, Moore TW, Yoon Y, Prussia A, Maddox C, Liotta DC, Shim H, Snyder JP.. (2013) Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.. J Med Chem, 56 (9): (3456-3466). [PMID:23550937] [10.1021/jm4002692] |
| 64. Lin WH, Hsu JT, Hsieh SY, Chen CT, Song JS, Yen SC, Hsu T, Lu CT, Chen CH, Chou LH, Yang YN, Chiu CH, Chen CP, Tseng YJ, Yen KJ, Yeh CF, Chao YS, Yeh TK, Jiaang WT.. (2013) Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).. Bioorg Med Chem, 21 (11): (2856-2867). [PMID:23618709] [10.1016/j.bmc.2013.03.083] |
| 65. Banappagari S, McCall A, Fontenot K, Vicente MG, Gujar A, Satyanarayanajois S.. (2013) Design, synthesis and characterization of peptidomimetic conjugate of BODIPY targeting HER2 protein extracellular domain.. Eur J Med Chem, 65 (60-69). [PMID:23688700] [10.1016/j.ejmech.2013.04.038] |
| 66. Zhou W, Liu X, Tu Z, Zhang L, Ku X, Bai F, Zhao Z, Xu Y, Ding K, Ding K, Li H.. (2013) Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant.. J Med Chem, 56 (20): (7821-7837). [PMID:24053674] [10.1021/jm401045n] |
| 67. Nesi G, Sestito S, Mey V, Ricciardi S, Falasca M, Danesi R, Lapucci A, Breschi MC, Fogli S, Rapposelli S.. (2013) Synthesis of Novel 3,5-Disubstituted-2-oxindole Derivatives As Antitumor Agents against Human Nonsmall Cell Lung Cancer.. ACS Med Chem Lett, 4 (12): (1137-1141). [PMID:24900620] [10.1021/ml400162g] |
| 68. Sridhar J, Sfondouris ME, Bratton MR, Nguyen TL, Townley I, Klein Stevens CL, Jones FE.. (2014) Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.. Bioorg Med Chem Lett, 24 (1): (126-131). [PMID:24355130] [10.1016/j.bmcl.2013.11.064] |
| 69. Cheng H, Chang Y, Zhang L, Luo J, Tu Z, Lu X, Zhang Q, Lu J, Ren X, Ding K, Ding K.. (2014) Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.. J Med Chem, 57 (6): (2692-2703). [PMID:24588073] [10.1021/jm500007h] |
| 70. Szokol B, Gyulavári P, Kurkó I, Baska F, Szántai-Kis C, Greff Z, Orfi Z, Peták I, Pénzes K, Torka R, Ullrich A, Orfi L, Vántus T, Kéri G.. (2014) Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.. ACS Med Chem Lett, 5 (4): (298-303). [PMID:24900830] [10.1021/ml4003309] |
| 71. Sangani CB, Makawana JA, Duan YT, Yin Y, Teraiya SB, Thumar NJ, Zhu HL.. (2014) Design, synthesis and molecular modeling of biquinoline-pyridine hybrids as a new class of potential EGFR and HER-2 kinase inhibitors.. Bioorg Med Chem Lett, 24 (18): (4472-4476). [PMID:25172421] [10.1016/j.bmcl.2014.07.094] |
| 72. Lawrence HR, Mahajan K, Luo Y, Zhang D, Tindall N, Huseyin M, Gevariya H, Kazi S, Ozcan S, Mahajan NP, Lawrence NJ.. (2015) Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.. J Med Chem, 58 (6): (2746-2763). [PMID:25699576] [10.1021/jm501929n] |
| 73. Lin XD, Yang HW, Ma S, Li WW, Zhang CH, Wang WJ, Xiang R, Li LL, Yang SY.. (2015) Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.. Bioorg Med Chem Lett, 25 (20): (4534-4538). [PMID:26342867] [10.1016/j.bmcl.2015.08.068] |
| 74. Elkamhawy A, Farag AK, Viswanath AN, Bedair TM, Leem DG, Lee KT, Pae AN, Roh EJ.. (2015) Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.. Bioorg Med Chem Lett, 25 (22): (5147-5154). [PMID:26475520] [10.1016/j.bmcl.2015.10.003] |
| 75. Qin M, Wang T, Xu B, Ma Z, Jiang N, Xie H, Gong P, Zhao Y.. (2015) Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant.. Eur J Med Chem, 104 (115-126). [PMID:26451770] [10.1016/j.ejmech.2015.09.031] |
| 76. Simon-Szabó L, Kokas M, Greff Z, Boros S, Bánhegyi P, Zsákai L, Szántai-Kis C, Vantus T, Mandl J, Bánhegyi G, Vályi-Nagy I, Őrfi L, Ullrich A, Csala M, Kéri G.. (2016) Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes.. Bioorg Med Chem Lett, 26 (2): (424-428). [PMID:26704265] [10.1016/j.bmcl.2015.11.099] |
| 77. Jung ME, Byun BJ, Kim HM, Lee JY, Park JH, Lee N, Son YH, Choi SU, Yang KM, Kim SJ, Lee K, Kim YC, Choi G.. (2016) Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.. Bioorg Med Chem Lett, 26 (11): (2719-2723). [PMID:27106709] [10.1016/j.bmcl.2016.03.111] |
| 78. Daydé-Cazals B, Fauvel B, Singer M, Feneyrolles C, Bestgen B, Gassiot F, Spenlinhauer A, Warnault P, Van Hijfte N, Borjini N, Chevé G, Yasri A.. (2016) Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.. J Med Chem, 59 (8): (3886-3905). [PMID:27010810] [10.1021/acs.jmedchem.6b00087] |
| 79. Schroeder RL, Goyal N, Bratton M, Townley I, Pham NA, Tram P, Stone T, Geathers J, Nguyen K, Sridhar J.. (2016) Identification of quinones as novel PIM1 kinase inhibitors.. Bioorg Med Chem Lett, 26 (13): (3187-3191). [PMID:27173800] [10.1016/j.bmcl.2016.04.079] |
| 80. Tantak MP, Gupta V, Nikhil K, Arun V, Singh RP, Jha PN, Shah K, Kumar D.. (2016) Sequential one-pot synthesis of bis(indolyl)glyoxylamides: Evaluation of antibacterial and anticancer activities.. Bioorg Med Chem Lett, 26 (13): (3167-3171). [PMID:27173802] [10.1016/j.bmcl.2016.04.080] |
| 81. Yin S, Tang C, Wang B, Zhang Y, Zhou L, Xue L, Zhang C.. (2016) Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.. Eur J Med Chem, 120 (26-36). [PMID:27187856] [10.1016/j.ejmech.2016.04.072] |
| 82. Shi Y, Park J, Lagisetti C, Zhou W, Sambucetti LC, Webb TR.. (2017) A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.. Bioorg Med Chem Lett, 27 (3): (406-412). [PMID:28049589] [10.1016/j.bmcl.2016.12.056] |
| 83. Hamed MM, Darwish SS, Herrmann J, Abadi AH, Engel M.. (2017) First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents.. J Med Chem, 60 (7): (2853-2868). [PMID:28291344] [10.1021/acs.jmedchem.6b01774] |
| 84. Zhu W, Chen H, Wang Y, Wang J, Peng X, Chen X, Gao Y, Li C, He Y, Ai J, Geng M, Zheng M, Liu H.. (2017) Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.. J Med Chem, 60 (14): (6018-6035). [PMID:28714692] [10.1021/acs.jmedchem.7b00076] |
| 85. Crawford JJ, Johnson AR, Misner DL, Belmont LD, Castanedo G, Choy R, Coraggio M, Dong L, Eigenbrot C, Erickson R, Ghilardi N, Hau J, Katewa A, Kohli PB, Lee W, Lubach JW, McKenzie BS, Ortwine DF, Schutt L, Tay S, Wei B, Reif K, Liu L, Wong H, Young WB.. (2018) Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.. J Med Chem, 61 (6): (2227-2245). [PMID:29457982] [10.1021/acs.jmedchem.7b01712] |
| 86. Wang A, Li X, Wu H, Zou F, Yan XE, Chen C, Hu C, Yu K, Wang W, Zhao P, Wu J, Qi Z, Wang W, Wang B, Wang L, Ren T, Zhang S, Yun CH, Liu J, Liu Q.. (2017) Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.. J Med Chem, 60 (7): (2944-2962). [PMID:28282122] [10.1021/acs.jmedchem.6b01907] |
| 87. Juchum M, Günther M, Döring E, Sievers-Engler A, Lämmerhofer M, Laufer S.. (2017) Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping.. J Med Chem, 60 (11): (4636-4656). [PMID:28482151] [10.1021/acs.jmedchem.7b00178] |
| 88. He L, Li D, Zhang C, Bai P, Chen L.. (2017) Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.. Bioorg Med Chem Lett, 27 (17): (4171-4175). [PMID:28734581] [10.1016/j.bmcl.2017.07.009] |
| 89. Malki WH, Gouda AM, Ali HEA, Al-Rousan R, Samaha D, Abdalla AN, Bustamante J, Abd Elmageed ZY, Ali HI.. (2018) Structural-based design, synthesis, and antitumor activity of novel alloxazine analogues with potential selective kinase inhibition.. Eur J Med Chem, 152 (31-52). [PMID:29684708] [10.1016/j.ejmech.2018.04.029] |
| 90. Monastyrskyi A, Nilchan N, Quereda V, Noguchi Y, Ruiz C, Grant W, Cameron M, Duckett D, Roush W.. (2018) Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.. Bioorg Med Chem, 26 (3): (590-602). [PMID:29289448] [10.1016/j.bmc.2017.12.020] |
| 91. La Pietra V, Sartini S, Botta L, Antonelli A, Ferrari SM, Fallahi P, Moriconi A, Coviello V, Quattrini L, Ke YY, Hsing-Pang H, Da Settimo F, Novellino E, La Motta C, Marinelli L.. (2018) Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.. Eur J Med Chem, 150 (491-505). [PMID:29549836] [10.1016/j.ejmech.2018.02.080] |
| 92. Hossam M, Lasheen DS, Ismail NSM, Esmat A, Mansour AM, Singab ANB, Abouzid KAM.. (2018) Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity.. Eur J Med Chem, 144 (330-348). [PMID:29275232] [10.1016/j.ejmech.2017.12.022] |
| 93. Liu H, Liang H, Meng H, Deng X, Zhang X, Lai L.. (2018) A novel allosteric inhibitor that prevents IKKβ activation.. Medchemcomm, 9 (2): (239-243). [PMID:30108917] [10.1039/C7MD00599G] |
| 94. Naik H, Gauthier T, Singh S, Jois S.. (2018) Design of novel lipidated peptidomimetic conjugates for targeting EGFR heterodimerization in HER2 + cancer.. Bioorg Med Chem Lett, 28 (22): (3506-3513). [PMID:30314880] [10.1016/j.bmcl.2018.10.005] |
| 95. Zhang Y, Lv H, Luo L, Xu Y, Pan Y, Wang Y, Lin H, Xiong J, Guo P, Zhang J, Li X, Ye F.. (2018) Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer.. Eur J Med Chem, 157 (1300-1325). [PMID:30195240] [10.1016/j.ejmech.2018.08.031] |
| 96. Milik SN, Lasheen DS, Serya RAT, Abouzid KAM.. (2017) How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.. Eur J Med Chem, 142 (131-151). [PMID:28754471] [10.1016/j.ejmech.2017.07.023] |
| 97. Ju Y, Wu J, Yuan X, Zhao L, Zhang G, Li C, Qiao R.. (2018) Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.. J Med Chem, 61 (24): (11372-11383). [PMID:30508379] [10.1021/acs.jmedchem.8b01612] |
| 98. Das D, Xie L, Wang J, Xu X, Zhang Z, Shi J, Le X, Hong J.. (2019) Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1.. Bioorg Med Chem Lett, 29 (4): (591-596). [PMID:30600209] [10.1016/j.bmcl.2018.12.056] |
| 99. Zhang C, Pei H, He J, Zhu J, Li W, Niu T, Xiang M, Chen L.. (2019) Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.. Eur J Med Chem, 169 (121-143). [PMID:30875504] [10.1016/j.ejmech.2019.02.077] |
| 100. Gavriil ES, Doukatas A, Karampelas T, Myrianthopoulos V, Dimitrakis S, Mikros E, Marakos P, Tamvakopoulos C, Pouli N.. (2019) Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.. Eur J Med Chem, 176 (393-409). [PMID:31125894] [10.1016/j.ejmech.2019.05.029] |
| 101. Wang Y, Li L, Fan J, Dai Y, Jiang A, Geng M, Ai J, Duan W.. (2018) Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.. J Med Chem, 61 (20): (9085-9104). [PMID:29522671] [10.1021/acs.jmedchem.7b01843] |
| 102. Saha T, Makar S, Swetha R, Gutti G, Singh SK.. (2019) Estrogen signaling: An emanating therapeutic target for breast cancer treatment.. Eur J Med Chem, 177 (116-143). [PMID:31129450] [10.1016/j.ejmech.2019.05.023] |
| 103. Wang Q, Dai Y, Ji Y, Shi H, Guo Z, Chen D, Chen Y, Peng X, Gao Y, Wang X, Chen L, Jiang Y, Geng M, Shen J, Ai J, Xiong B.. (2019) Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma.. Eur J Med Chem, 163 (671-689). [PMID:30572178] [10.1016/j.ejmech.2018.12.015] |
| 104. Guo Y, Liu Y, Hu N, Yu D, Zhou C, Shi G, Zhang B, Wei M, Liu J, Luo L, Tang Z, Song H, Guo Y, Liu X, Su D, Zhang S, Song X, Zhou X, Hong Y, Chen S, Cheng Z, Young S, Wei Q, Wang H, Wang Q, Lv L, Wang F, Xu H, Sun H, Xing H, Li N, Zhang W, Wang Z, Liu G, Sun Z, Zhou D, Li W, Liu L, Wang L, Wang Z.. (2019) Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.. J Med Chem, 62 (17): (7923-7940). [PMID:31381333] [10.1021/acs.jmedchem.9b00687] |
| 105. Lin SY, Chang Hsu Y, Peng YH, Ke YY, Lin WH, Sun HY, Shiao HY, Kuo FM, Chen PY, Lien TW, Chen CH, Chu CY, Wang SY, Yeh KC, Chen CP, Hsu TA, Wu SY, Yeh TK, Chen CT, Hsieh HP.. (2019) Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.. J Med Chem, 62 (22): (10108-10123). [PMID:31560541] [10.1021/acs.jmedchem.9b00722] |
| 106. Mansour TS, Pallepati RR, Basetti V.. (2020) Potent dual EGFR/Her4 tyrosine kinase inhibitors containing novel (1,2-dithiolan-4-yl)acetamides.. Bioorg Med Chem Lett, 30 (16): (127288-127288). [PMID:32631510] [10.1016/j.bmcl.2020.127288] |
| 107. Pulz R,Angst D,Dawson J,Gessier F,Gutmann S,Hersperger R,Hinniger A,Janser P,Koch G,Revesz L,Vulpetti A,Waelchli R,Zimmerlin A,Cenni B. (2019) Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.. ACS Med Chem Lett, 10 (10.0): (1467-1472). [PMID:31620235] [10.1021/acsmedchemlett.9b00317] |
| 108. Lategahn J,Hardick J,Grabe T,Niggenaber J,Jeyakumar K,Keul M,Tumbrink HL,Becker C,Hodson L,Kirschner T,Klövekorn P,Ketzer J,Baumann M,Terheyden S,Unger A,Weisner J,Müller MP,van Otterlo WAL,Bauer S,Rauh D. (2020) Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.. J Med Chem, 63 (20.0): (11725-11755). [PMID:32931277] [10.1021/acs.jmedchem.0c00870] |
| 109. Baillache, Daniel J., Unciti-Broceta, Asier. (2020) Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold. RSC Med Chem, 11 (10): (1112-1135). [PMID:33479617] [10.1039/d0md00227e] |
| 110. Shu L,Chen C,Huan X,Huang H,Wang M,Zhang J,Yan Y,Liu J,Zhang T,Zhang D. (2020) Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.. Eur J Med Chem, 191 (112148-112148). [PMID:32097841] [10.1016/j.ejmech.2020.112148] |
| 111. Elseginy SA,Hamdy R,Menon V,Almehdi AM,El-Awady R,Soliman SSM. (2020) Design, synthesis, and computational validation of novel compounds selectively targeting HER2-expressing breast cancer.. Bioorg Med Chem Lett, 30 (24): (127658-127658). [PMID:33130288] [10.1016/j.bmcl.2020.127658] |
| 112. Ebrahim HY,Mohyeldin MM,Hailat MM,El Sayed KA. (2016) (1S,2E,4S,7E,11E)-2,7,11-Cembratriene-4,6-diol semisynthetic analogs as novel c-Met inhibitors for the control of c-Met-dependent breast malignancies.. Bioorg Med Chem, 24 (22.0): (5748-5761). [PMID:27681240] [10.1016/j.bmc.2016.09.032] |
| 113. He L,Pei H,Zhang C,Shao M,Li D,Tang M,Wang T,Chen X,Xiang M,Chen L. (2018) Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.. Eur J Med Chem, 145 (96-112). [PMID:29324347] [10.1016/j.ejmech.2017.12.079] |
| 114. Elwaie TA,Abbas SE,Aly EI,George RF,Ali H,Kraiouchkine N,Abdelwahed KS,Fandy TE,El Sayed KA,Abd Elmageed ZY,Ali HI. (2020) HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability.. J Med Chem, 63 (24.0): (15906-15945). [PMID:33314925] [10.1021/acs.jmedchem.0c01647] |
| 115. Zhao L,Fan T,Shi Z,Ding C,Zhang C,Yuan Z,Sun Q,Tan C,Chu B,Jiang Y. (2021) Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR mutant cell lines.. Eur J Med Chem, 213 (113173-113173). [PMID:33493830] [10.1016/j.ejmech.2021.113173] |
| 116. Lamie PF,El-Kalaawy AM,Abdel Latif NS,Rashed LA,Philoppes JN. (2021) Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.. Eur J Med Chem, 214 (113222-113222). [PMID:33545637] [10.1016/j.ejmech.2021.113222] |
| 117. Pang H,Wang N,Chai J,Wang X,Zhang Y,Bi Z,Wu W,He G. (2020) Discovery of novel TNNI3K inhibitor suppresses pyroptosis and apoptosis in murine myocardial infarction injury.. Eur J Med Chem, 197 (112314-112314). [PMID:32344181] [10.1016/j.ejmech.2020.112314] |
| 118. Lakkaniga NR,Zhang L,Belachew B,Gunaganti N,Frett B,Li HY. (2020) Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression.. Eur J Med Chem, 203 (112589-112589). [PMID:32717530] [10.1016/j.ejmech.2020.112589] |
| 119. Singh SS, Mattheolabakis G, Gu X, Withers S, Dahal A, Jois S.. (2021) A grafted peptidomimetic for EGFR heterodimerization inhibition: Implications in NSCLC models.. Eur J Med Chem, 216 (113312-113312). [PMID:33667849] [10.1016/j.ejmech.2021.113312] |
| 120. King, C R CR, Kraus, M H MH and Aaronson, S A SA.. (1985) Amplification of a novel v-erbB-related gene in a human mammary carcinoma.. Science (New York, N.Y.), (6): [PMID:2992089] |
| 121. Semba, K K, Kamata, N N, Toyoshima, K K and Yamamoto, T T.. (1985) A v-erbB-related protooncogene, c-erbB-2, is distinct from the c-erbB-1/epidermal growth factor-receptor gene and is amplified in a human salivary gland adenocarcinoma.. Proceedings of the National Academy of Sciences of the United States of America, [PMID:2995967] |
| 122. Coussens, L L and 9 more authors.. (1985) Tyrosine kinase receptor with extensive homology to EGF receptor shares chromosomal location with neu oncogene.. Science (New York, N.Y.), (6): [PMID:2999974] |
| 123. Yamamoto, T T and 7 more authors.. (1986) Similarity of protein encoded by the human c-erb-B-2 gene to epidermal growth factor receptor.. Nature, [PMID:3003577] |
| 124. Tal, M M and 5 more authors.. (1987) Human HER2 (neu) promoter: evidence for multiple mechanisms for transcriptional initiation.. Molecular and cellular biology, [PMID:3039351] |
| 125. Ehsani, A A, Low, J J, Wallace, R B RB and Wu, A M AM.. (1993) Characterization of a new allele of the human ERBB2 gene by allele-specific competition hybridization.. Genomics, [PMID:8095488] |
| 126. Sarkar, F H FH, Ball, D E DE, Li, Y W YW and Crissman, J D JD.. (1993) Molecular cloning and sequencing of an intron of Her-2/neu (ERBB2) gene.. DNA and cell biology, [PMID:8104414] |
| 127. Olayioye, M A MA, Beuvink, I I, Horsch, K K, Daly, J M JM and Hynes, N E NE.. (1999) ErbB receptor-induced activation of stat transcription factors is mediated by Src tyrosine kinases.. The Journal of biological chemistry, (11): [PMID:10358079] |
| 128. Kuhns, J J JJ, Batalia, M A MA, Yan, S S and Collins, E J EJ.. (1999) Poor binding of a HER-2/neu epitope (GP2) to HLA-A2.1 is due to a lack of interactions with the center of the peptide.. The Journal of biological chemistry, (17): [PMID:10593938] |
| 129. Treish, I I, Schwartz, R R and Lindley, C C.. (2000) Pharmacology and therapeutic use of trastuzumab in breast cancer.. American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, (15): [PMID:11098307] |
| 130. Birrane, Gabriel G, Chung, Judy J and Ladias, John A A JA.. (2003) Novel mode of ligand recognition by the Erbin PDZ domain.. The Journal of biological chemistry, (17): [PMID:12444095] |
| 131. Li, Yongqing Y and 7 more authors.. (2003) Heregulin targets gamma-catenin to the nucleolus by a mechanism dependent on the DF3/MUC1 oncoprotein.. Molecular cancer research : MCR, [PMID:12939402] |
| 132. Ivancic, Monika M, Daly, Roger J RJ and Lyons, Barbara A BA.. (2003) Solution structure of the human Grb7-SH2 domain/erbB2 peptide complex and structural basis for Grb7 binding to ErbB2.. Journal of biomolecular NMR, [PMID:12975581] |
| 133. Xia, Wenle W, Liu, Lei-Hua LH, Ho, Peter P and Spector, Neil L NL.. (2004) Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016.. Oncogene, (22): [PMID:14737100] |
| 134. Marone, Romina R and 5 more authors.. (2004) Memo mediates ErbB2-driven cell motility.. Nature cell biology, [PMID:15156151] |
| 135. and Burris, Howard A HA.. (2004) Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib.. The oncologist, [PMID:15163842] |
| 136. Swiercz, Jakub M JM, Kuner, Rohini R and Offermanns, Stefan S.. (2004) Plexin-B1/RhoGEF-mediated RhoA activation involves the receptor tyrosine kinase ErbB-2.. The Journal of cell biology, (21): [PMID:15210733] |
| 137. Wang, Shao-Chun SC and 11 more authors.. (2004) Binding at and transactivation of the COX-2 promoter by nuclear tyrosine kinase receptor ErbB-2.. Cancer cell, [PMID:15380516] |
| 138. Stephens, Philip P and 59 more authors.. (2004) Lung cancer: intragenic ERBB2 kinase mutations in tumours.. Nature, (30): [PMID:15457249] |
| 139. Giri, Dipak K DK and 7 more authors.. (2005) Endosomal transport of ErbB-2: mechanism for nuclear entry of the cell surface receptor.. Molecular and cellular biology, [PMID:16314522] |
| 140. Anido, Judit J and 6 more authors.. (2006) Biosynthesis of tumorigenic HER2 C-terminal fragments by alternative initiation of translation.. The EMBO journal, (12): [PMID:16794579] |
| 141. Johnston, Stephen R D SR and Leary, Alex A.. (2006) Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer.. Drugs of today (Barcelona, Spain : 1998), [PMID:16894399] |
| 142. Farhan, Hesso H and 9 more authors.. (2006) Inhibition of xenograft tumor growth and down-regulation of ErbB receptors by an antibody directed against Lewis Y antigen.. The Journal of pharmacology and experimental therapeutics, [PMID:16963623] |
| 143. Deng, Suhua S and 11 more authors.. (2007) Plexin-B2, but not Plexin-B1, critically modulates neuronal migration and patterning of the developing nervous system in vivo.. The Journal of neuroscience : the official journal of the Society for Neuroscience, (6): [PMID:17554007] |
| 144. Lin, Amy A and Rugo, Hope S HS.. (2007) The role of trastuzumab in early stage breast cancer: current data and treatment recommendations.. Current treatment options in oncology, [PMID:17660958] |
| 145. Levêque, Dominique D, Gigou, Luc L and Bergerat, Jean Pierre JP.. (2008) Clinical pharmacology of trastuzumab.. Current clinical pharmacology, [PMID:18690878] |
| 146. Xiang, Bin B and 8 more authors.. (2008) Brk is coamplified with ErbB2 to promote proliferation in breast cancer.. Proceedings of the National Academy of Sciences of the United States of America, (26): [PMID:18719096] |
| 147. Medina, Patrick J PJ and Goodin, Susan S.. (2008) Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases.. Clinical therapeutics, [PMID:18803986] |
| 148. Hawthorne, Valerie S VS and 5 more authors.. (2009) ErbB2-mediated Src and signal transducer and activator of transcription 3 activation leads to transcriptional up-regulation of p21Cip1 and chemoresistance in breast cancer cells.. Molecular cancer research : MCR, [PMID:19372587] |
| 149. Heinrich, C C and 9 more authors.. (2010) Copine-III interacts with ErbB2 and promotes tumor cell migration.. Oncogene, (18): [PMID:20010870] |
| 150. Tevaarwerk, Amye J AJ and Kolesar, Jill M JM.. (2009) Lapatinib: a small-molecule inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor-2 tyrosine kinases used in the treatment of breast cancer.. Clinical therapeutics, [PMID:20110044] |
| 151. Vazquez-Martin, Alejandro A and 5 more authors.. (2011) Lapatinib, a dual HER1/HER2 tyrosine kinase inhibitor, augments basal cleavage of HER2 extracellular domain (ECD) to inhibit HER2-driven cancer cell growth.. Journal of cellular physiology, [PMID:20658522] |
| 152. Eigenbrot, Charles C, Ultsch, Mark M, Dubnovitsky, Anatoly A, Abrahmsén, Lars L and Härd, Torleif T.. (2010) Structural basis for high-affinity HER2 receptor binding by an engineered protein.. Proceedings of the National Academy of Sciences of the United States of America, (24): [PMID:20696930] |
| 153. Zaoui, Kossay K, Benseddik, Khedidja K, Daou, Pascale P, Salaün, Danièle D and Badache, Ali A.. (2010) ErbB2 receptor controls microtubule capture by recruiting ACF7 to the plasma membrane of migrating cells.. Proceedings of the National Academy of Sciences of the United States of America, (26): [PMID:20937854] |
| 154. Zang, Zhi Jiang ZJ and 18 more authors.. (2011) Genetic and structural variation in the gastric cancer kinome revealed through targeted deep sequencing.. Cancer research, (1): [PMID:21097718] |
| 155. Kharmate, Geetanjali G and 6 more authors.. (2011) Dissociation of epidermal growth factor receptor and ErbB2 heterodimers in the presence of somatostatin receptor 5 modulate signaling pathways.. Endocrinology, [PMID:21190959] |
| 156. Li, Long-Yuan LY and 14 more authors.. (2011) Nuclear ErbB2 enhances translation and cell growth by activating transcription of ribosomal RNA genes.. Cancer research, (15): [PMID:21555369] |
| 157. Barginear, Myra F MF, John, Veena V and Budman, Daniel R DR.. (2013) Trastuzumab-DM1: a clinical update of the novel antibody-drug conjugate for HER2-overexpressing breast cancer.. Molecular medicine (Cambridge, Mass.), (22): [PMID:23196784] |
| 158. Corominas, Roser R and 29 more authors.. (2014) Protein interaction network of alternatively spliced isoforms from brain links genetic risk factors for autism.. Nature communications, (11): [PMID:24722188] |
| 159. Li, Hui H and 18 more authors.. (2016) Crystal Structure and Substrate Specificity of PTPN12.. Cell reports, (10): [PMID:27134172] |
| 160. Borges, Virginia F VF and 13 more authors.. (2018) Tucatinib Combined With Ado-Trastuzumab Emtansine in Advanced ERBB2/HER2-Positive Metastatic Breast Cancer: A Phase 1b Clinical Trial.. JAMA oncology, (1): [PMID:29955792] |
| 161. Tam, Constantine Si Lun CSL and 20 more authors.. (2019) Phase 1 study of selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL.. Blood, (24): [PMID:31340982] |
| 162. Li, Hui and 11 more authors.. (2020) SH3BGRL confers innate drug resistance in breast cancer by stabilizing HER2 activation on cell membrane.. Journal of experimental & clinical cancer research : CR, (7): [PMID:32381043] |
| 163. Le, Thuy-Linh and 36 more authors.. (2021) Dysregulation of the NRG1-ERBB pathway causes a developmental disorder with gastrointestinal dysmotility in humans.. The Journal of clinical investigation, (26): [PMID:33497358] |
| 164. Arcaro, A A and 5 more authors.. (2000) Class II phosphoinositide 3-kinases are downstream targets of activated polypeptide growth factor receptors.. Molecular and cellular biology, [PMID:10805725] |
| 165. Chen, X X, Ji, Z L ZL and Chen, Y Z YZ.. (2002) TTD: Therapeutic Target Database.. Nucleic acids research, (1): [PMID:11752352] |
| 166. Yin L, Li H, Liu W, Yao Z, Cheng Z, Zhang H, Zou H. (2018) A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.. Eur J Med Chem, 144 (1-28). [PMID:29247857] |
| 167. Sandra N Milik,Amal Kamal Abdel-Aziz,Deena S Lasheen,Rabah A T Serya,Saverio Minucci,Khaled A M Abouzid. (2018-06-15) Surmounting the resistance against EGFR inhibitors through the development of thieno[2,3-d]pyrimidine-based dual EGFR/HER2 inhibitors.. European journal of medicinal chemistry, 155 (316-336). [PMID:29902719] |
首页
400-620-6333
