BS181
| 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
| 储存条件 | under inert gas (nitrogen or Argon) at 2–8 °C |
|---|---|
| 溶解度 | 不溶于水； DMSO 中≥20.85 mg/mL； ≥6.49 mg/mL，乙醇溶液，超声波 |
| 形态 | 固体 |
|
CDK7/CycH/MAT1 0.021 μM (IC 50 ) |
CDK2/Cyc E 0.88 μM (IC 50 ) |
CDK5/p35NCK 3 μM (IC 50 ) |
CDK9/cycT 4.2 μM (IC 50 ) |
CDK1/cycB 8.1 μM (IC 50 ) |
CDK4/Cyc D1 33 μM (IC 50 ) |
CDK6/cycD1 47 μM (IC 50 ) |
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.
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.