名称 | JH-VIII-157-02 |
描述 | JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L. |
体外活性 | JH-VIII-157-02 potently inhibits EML4-ALKS1206Y, EML4-ALKG1269A, EML4-ALKL1196M, EML4-ALK1151Tins, and EML4-ALKL1152R with IC50s of 2, 3, 58, 107 and 196 nM, respectively. JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4 with IC50s of 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM, respectively[1]. |
体内活性 | In mice, JH-VIII-157-02 (10 mg/kg) exhibits good oral bioavailability and penetrates the central nervous system[1]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 25 mg/mL (53.70 mM)
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关键字 | JH-VIII-157-02 | JHVIII15702 | JH VIII 157 02 | Inhibitor | inhibit | Cluster of differentiation 246 | CD246 | Anaplastic lymphoma kinase (ALK) | Anaplastic lymphoma kinase | ALK tyrosine kinase receptor |
相关产品 | Flubendazole | Mebendazole | N-Phenylbenzylamine | 4-Isopropoxybenzoic acid | Oxfendazole | Thiabendazole | Methylene Blue | Methylene Blue trihydrate | Griseofulvin | Paclitaxel | A 83-01 | 4'-Demethylepipodophyllotoxin |
相关库 | 抗肺癌化合物库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库 | 激酶抑制剂库 | 微管靶向化合物库 | 血管生成库 | 抑制剂库 | 已知活性化合物库 | 共价抑制剂库 | 细胞骨架化合物库 |