ChemicalBook > CAS DataBase List > BS-181 hydrochloride
BS-181 hydrochloride
BS-181 hydrochloride
- CAS No.1092443-52-1
- Chemical Name:BS-181 hydrochloride
- CBNumber:CB42561462
- Molecular Formula:C22H32N6
- Formula Weight:380.53
- MOL File:1092443-52-1.mol
BS-181 hydrochloride Property
- Density 1.16
- storage temp. Store at -20°C
- solubility Soluble in DMSO
- form Powder
- pka 10.62±0.10(Predicted)
- color White to off-white
- FDA UNII 75M620LLBN
- Symbol(GHS)
- Signal word
- Hazard statements
- Precautionary statements
BS-181 hydrochloride Chemical Properties,Usage,Production
- Uses BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy[1][2].
- Definition ChEBI: N5-(6-aminohexyl)-N7-(phenylmethyl)-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine is a pyrazolopyrimidine.
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in vivo
BS-181 (intraperitoneal injection; 5 mg/kg or 10 mg/kg twice daily; total daily doses of 10 mg/kg or 20 mg/kg; 14 days) inhibitstumor growth in a dose-dependent manner.?Tumor growth exhibits 25% and 50% reduction compared with the control group, for 10 mg/kg/day and 20 mg/kg/day, respectively[1].
Animal Model: 7-week old female nu/nu-BALB/c athymic nude mice?with MCF-7 cells[1] Dosage: 5 mg/kg or 10 mg/kg; 10 mg/kg or 20 mg/kg Administration: Intraperitoneal injection; twice daily or once total daily; 14 days Result: Inhibited tumor growth significantly. - IC 50 CDK7/CycH/MAT1: 0.021 μM (IC50); CDK2/Cyc E: 0.88 μM (IC50); CDK5/p35NCK: 3 μM (IC50); CDK9/cycT: 4.2 μM (IC50); CDK1/cycB: 8.1 μM (IC50); CDK4/Cyc D1: 33 μM (IC50); CDK6/cycD1: 47 μM (IC50)
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References
[1] Ali S et al. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009 Aug 1;69(15):6208-15. DOI:10.1158/0008-5472.CAN-09-0301
[2] Wang BY, et al. Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer. Drug Des Devel Ther. 2016 Mar 16;10:1181-9. DOI:10.2147/DDDT.S86317
BS-181 hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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- Inhibitors
- 细胞生物学试剂
- 小分子抑制剂,天然产物
- 小分子抑制剂
- 细胞周期
- 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
- BS-181,CDK7抑制剂
- 化合物BS-181
- CDK7抑制剂(BS-181)
- N5-(6-氨基己基)-3-异丙基-N7-苄基吡唑并[1,5-A]嘧啶-5,7-二胺
- 1092443-52-1
- Pyrazolo[1,5-a]pyrimidine-5,7-diamine, N5-(6-aminohexyl)-3-(1-methylethyl)-N7-(phenylmethyl)-
- 5-N-(6-aminohexyl)-7-N-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine,hydrochloride
- CS-507
- CS-2137
- BS-181 free base
- BS-181 HCl
- N5-(6-Aminohexyl)-3-isopropyl-N7-benzylpyrazolo[1,5-a]pyrimidine-5,7-diamine
- BS 181
- BS-181 hydrochloride