BS181 CAS#: 1397219-81-6

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BS181

生物活性靶点体外研究体内研究

中文名称	BS181
中文同义词	BS-181 盐酸盐;化合物BS-181 HCL;N5-(6-氨基己基)-N7-苄基-3-异丙基吡唑并[1,5-A]嘧啶-5,7-二胺盐酸盐;BS-181盐酸
英文名称	BS-181 HCl
英文同义词	N5-(6-aminohexyl)-N7-benzyl-3-isopropylpyrazolo[1,5-a]pyrimidine-5,7-diamine hydrochloride;BS181;BS 181;CS-979;BS-181 HCl USP/EP/BP
CAS号	1397219-81-6
分子式	C22H33ClN6
分子量	416.99062
EINECS号
相关类别	小分子抑制剂，天然产物;生物活性分子;Inhibitors
Mol文件	1397219-81-6.mol
结构式

BS181 性质

BS181 用途与合成方法

生物活性

BS-181 hydrochloride 是一种高度选择性的 CDK7 抑制剂，IC50 值为 21 nM，对 CDK7 的选择性是对 CDK1，2，4，5，6 和 9 的 40 多倍。

靶点

体外研究

BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC     ₅₀    values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser     ⁷⁹⁵    and Ser     ⁸²¹    with an apparent IC     ₅₀    of 15 μM, similar to the IC     ₅₀    obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells leads to G1 arrest at and apoptosis. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC     ₅₀    ) ranging from 17 to 22 μM and 6.5 μM, respectively. BS-181 significantly inhibits cell migration and invasion ability in a dose-dependent manner.

体内研究

BS-181 (5 mg/kg, 10 mg/kg, i.p.) inhibits the growth of MCF-7 tumors in nude mice. Intravenous (i.v) and i.p administration of 10 mg/kg BS-181 shows rapid clearance. BS-181 (10 mg/kg/d or 20 mg/kg/d, i.p.) significantly inhibits the growth of tumor in a dose-dependent manner compared to the control group.

安全信息

MSDS信息

BS181 上下游产品信息