| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| I407799-1ml |
1ml |
现货  |
|
| 英文别名 | Gleevec, Glivec, CGP057148B | 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Imatinib (STI571) |
| 生化机理 | 伊马替尼（STI571，CGP057148B，格列卫）是一种多靶点酪氨酸激酶抑制剂，对 v-Abl、c-Kit 和 PDGFR 均有抑制作用，在无细胞或基于细胞的试验中，IC50 值分别为 0.6 μM、0.1 μM 和 0.1 μM。伊马替尼（STI571）诱导自噬。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | ABL 原癌基因 1 抑制剂；非受体酪氨酸激酶；盘状结构域受体酪氨酸激酶 1 抑制剂；盘状结构域受体酪氨酸激酶 2 抑制剂 |
| 产品介绍 |
Imatinib(STI571)是多靶点抑制剂，对 v-Abl，c-Kit和PDGFR的IC50分别为0.6 μM，0.1 μM和0.1 μM。An inhibitor of multiple tyrosine kinases Information Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor oftyrosine kinasewith inhibition forv-Abl,c-KitandPDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) inducesautophagy. In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis. In vivo Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation. cell lines： Concentrations：~100 μM Incubation Time：48 hours Powder Purity:≥99% |
| IC50 | v-Abl, IC50: 600 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CN1CCN(CC1)CC2=CC=C(C=C2)C(=O)NC3=CC=C(C)C(=C3)NC4=NC=CC(=N4)C5=CC=CN=C5 |
| 分子量 | 493.6 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 47 mg/mL (198.92 mM); Ethanol: 18 mg/mL (76.18 mM); Water: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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