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BS181
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基本信息
性质
用途
编辑结构
首页 化学性质 1397219-81-6
BS181
查看55 家供应商 暂无价格
CAS No. 1397219-81-6
分子式 C22H33ClN6
分子量 416.99062
英文名称 BS-181 HCl
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
基本信息
产品名称
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
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 No.
1397219-81-6
分子式
C22H33ClN6
分子量
416.99062
EINECS号
-
MDL NO.
MFCD18384975
性质
形态
solid
溶解度
insoluble in H2O; ≥20.85 mg/mL in DMSO; ≥6.49 mg/mL in EtOH with ultrasonic
储存条件
under inert gas (nitrogen or Argon) at 2–8 °C
用途
靶点
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 )
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.
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.
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。
编辑结构
15802146997 15001988657
中文名称:
BS181
英文名称:
BS-181 HCl
CAS NO.:
1397219-81-6
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13001525434 15988113297
中文名称:
BS181
英文名称:
BS-181 HCl
CAS NO.:
1397219-81-6
19945030958 027-027-59101668
中文名称:
BS181
英文名称:
BS-181 HCl
CAS NO.:
1397219-81-6
联系我们:
QQ
QQ号: 2881924765 复制
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微信洽谈
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