BS181
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 |
BS181 用途与合成方法
|
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.
