BS181
|
|
|
- CAS号:
- 1397219-81-6
- 英文名:
- BS-181 HCl
- 英文别名:
- CS-979;BS181;BS 181;BS-181 HCl USP/EP/BP;N5-(6-aminohexyl)-N7-benzyl-3-isopropylpyrazolo[1,5-a]pyrimidine-5,7-diamine hydrochloride
- 中文名:
- BS181
- 中文别名:
- BS-181盐酸;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
- CBNumber:
- CB22677402
- 分子式:
- C22H33ClN6
- 分子量:
- 416.99062
- MOL File:
- 1397219-81-6.mol
|
|
|
BS181化学性质
-
储存条件:
-
under inert gas (nitrogen or Argon) at 2–8 °C
-
|
-
溶解度:
-
insoluble in H2O; ≥20.85 mg/mL in DMSO; ≥6.49 mg/mL in EtOH with ultrasonic
-
|
-
形态:
-
solid
-
|
BS181性质、用途与生产工艺
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。
|
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.
BS181
上下游产品信息
上游原料
下游产品
1397219-81-6, BS181 相关搜索:
- Inhibitors
- 药靶配体
- 生物活性分子
- 小分子抑制剂，天然产物
- C22H32N6HCl
- BS-181盐酸
- 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
- 化合物BS-181 HCL
- BS-181 盐酸盐
- 1397219-81-6
- BS-181 HCl USP/EP/BP
- CS-979
- BS181;BS 181
- N5-(6-aminohexyl)-N7-benzyl-3-isopropylpyrazolo[1,5-a]pyrimidine-5,7-diamine hydrochloride