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1639422-97-1

中文名称 化合物 T15612
英文名称 JH-VIII-157-02
CAS 1639422-97-1
分子式 C28H27N5O2
分子量 465.55
MOL 文件 1639422-97-1.mol
更新日期 2024/02/18 09:39:49
1639422-97-1 结构式 1639422-97-1 结构式

基本信息

中文别名
化合物 T15612
英文别名
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-

物理化学性质

沸点751.9±60.0 °C(Predicted)
密度1.28±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO : ≥ 25 mg/mL (53.70 mM)
酸度系数(pKa)13.70±0.40(Predicted)
形态Solid
颜色White to off-white

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS07
警示词警告
危险性描述H302-H315-H319-H335
化合物 T15612价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-112140化合物 T15612
JH-VIII-157-02
1639422-97-11 mg1148元
2025/05/22HY-112140化合物 T15612
JH-VIII-157-02
1639422-97-15mg2988元
2025/05/22HY-112140化合物 T15612
JH-VIII-157-02
1639422-97-110 mM * 1 mLin DMSO3060元

常见问题列表

生物活性
JH-VIII-157-02 是 alectinib 的结构类似物,为 ALK 抑制剂,对棘皮动物微管相关蛋白样 4 (EML4)-ALK G1202R 的 IC50 值为 2 nM。
靶点

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)

体外研究

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.

体内研究

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.

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