JH-VIII-157-02

  • 10mM in DMSO
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
J655309-1ml
1ml 期货 Stock Image

基本描述

规格或纯度 10mM in DMSO
英文名称 JH-VIII-157-02
生化机理 JH-VIII-157-02是阿来替尼的结构类似物,是一种ALK抑制剂,对细胞中棘皮动物微管相关蛋白样4-ALK(EML4-ALK)G1202R的IC50为2 nM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍


JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC 50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.

In Vitro

JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC 50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. JH-VIII-157-02 also potently inhibits EML4-ALK wt (Eawt), EAC1156Y, EAF1174L, EAS1206Y (IC 50 , 2 nM), EAG1269A (IC 50 , 3 nM), EAL1196M (IC 50 , 58 nM), EA1151Tins (IC 50 , 107 nM), and EAL1152R (IC 50 , 196 nM). Moreover, JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4, and the IC 50 s are 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM respectively. JH-VIII-157-02 exhibits inhibitory growth of cancer cell lines, such as H3122, DFCI76 (L1152R] with EC 50 s of 5, 19 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JH-VIII-157-02 exhibits good oral bioavailability following an oral dose of 10 mg/kg in mice. JH-VIII-157-02 also penetrates the CNS of mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: 2 nM (EML4-ALK G1202R, cell assay), 2 nM (EML4-ALK wt , cell assay), 2 nM (EML4-ALK C1156Y, cell assay), 2 nM (EML4-ALK F1174L, cell assay), 2 nM (EML4-ALK F1174L, cell assay)

关联靶点(人)

RET Tclin 原癌基因酪氨酸蛋白激酶受体 Ret(Proto-oncogene tyrosine-protein kinase receptor Ret) (3 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
IRAK1 Tchem 白细胞介素-1受体相关激酶1(Interleukin-1 receptor-associated kinase 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ALK Tclin ALK 酪氨酸激酶受体(ALK tyrosine kinase receptor) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CLK4 Tchem 双特异性蛋白激酶 CLK4(Dual specificity protein kinase CLK4) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CCC1=CC2=C(C=C1C3=CN(N=C3)CC(=O)N(C)C)C(C4=C(C2=O)C5=C(N4)C=C(C=C5)C#N)(C)C
分子量 465.55

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