BS-181 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BS-181 是一种有效的选择性 CDK7 抑制剂，IC50 为 21 nM。

BS-181 is a potent, selective CDK7 inhibitor with IC50 of 21 nM, 40-fold selectivity over CDK2/cycE and no significant activity against CDK1/cycB, CDK4/cycD1, CDK5/p35NCK, CDK6/cycD1, and CDK9/cycT (IC50>1 uM); promotes cell cycle arrest and inhibits cancer cell growth in a panel of cell lines representing a range of tumor types (IC50=1.5 to 37 uM), inhibits the phosphorylation of CDK7 substrates, inhibits phosphorylation of the RNA polymerase II COOH-terminal domain (CTD) at P-Ser5 (IC50=9 uM), inhibits RB phosphorylation at Ser795 and Ser821 (IC50=15 uM); induces apoptosis in vitro, and shows antitumor effects in vivo.

BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC50 values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser795 and Ser821 with an apparent IC50 of 15 μM, similar to the IC50 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 (IC50) 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.

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.

BS181

Angiogenesis

CDK

CDK7

Cancer

——

1397219-81-6

417

C22H33ClN6

>98% (HPLC)

10 mM in DMSO

Cl.CC(C)C1=C2N=C(NCCCCCCN)C=C(NCC3=CC=CC=C3)N2N=C1 |c:3,21,23,28,t:5,15,19|

Pyrazolo[1,5-a]pyrimidine-5,7-diamine, N5-(6-aminohexyl)-3-(1-methylethyl)-N7-(phenylmethyl)-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years