化合物 T15612
| 中文名称 | 化合物 T15612 |
|---|---|
| 中文同义词 | 化合物 T15612;化合物JH-VIII-157-02;化合物JH-VIII-157-02,10 MM DMSO 溶液;2-(4-(3-氰基-9-乙基-6,6-二甲基-11-氧代-6,11-二氢-5H-苯并[b]咔唑-8-基)-1H-吡唑-1-基)-N,N-二甲基乙酰胺 |
| 英文名称 | JH-VIII-157-02 |
| 英文同义词 | JH-VIII-157-02;1H-Pyrazole-1-acetamide, 4-(3-cyano-9-ethyl-6,11-dihydro-6,6-dimethyl-11-oxo-5H-benzo[b]carbazol-8-yl)-N,N-dimethyl-;JH-VIII-157-02, 10 mM in DMSO;CD246,Cluster of differentiation 246,inhibit,Anaplastic lymphoma kinase,Anaplastic lymphoma kinase (ALK),ALK tyrosine kinase receptor,Inhibitor,JHVIII15702,JH VIII 157 02;2-(4-(3-Cyano-9-ethyl-6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazol-8-yl)-1H-pyrazol-1-yl)-N,N-dimethylacetamide |
| CAS号 | 1639422-97-1 |
| 分子式 | C28H27N5O2 |
| 分子量 | 465.55 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1639422-97-1.mol |
| 结构式 |  |
化合物 T15612 性质
| 沸点 | 751.9±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.28±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：≥ 25 mg/mL（53.70 mM） |
| 酸度系数(pKa) | 13.70±0.40(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
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)
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.
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-112140 | 化合物 T15612 JH-VIII-157-02 | 1639422-97-1 | 1 mg | 1148元 |
| 2025/12/22 | HY-112140 | 化合物 T15612 JH-VIII-157-02 | 1639422-97-1 | 5mg | 2988元 |