Cat. No. Name Size Price Add Cart
KI0534BS-181 HCl10 mg$512
BS-181 HCl50 mg$1552

Chemical Characteristic

Product NameBS-181 HCl
CAS No.1092443-52-1
Molecular Weight 380.53
FormulaC22H32N6
Chemical Name5-N-(6-aminohexyl)-7-N-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine
Smilesc12nc(cc(n1ncc2C(C)C)NCc1ccccc1)NCCCCCCN
Chemical Structure

Biological activities

BS-181 is a potent and selective CDK inhibitor. The IC50 value of BS-181 against CDK7 is 21 nM. The IC50 values of BS-181 against CDK1/cycB, CDK4/cycD1, CDK5/p35NCK, CDK6/cycD1 and CDK9/cycT are considerably higher than 1 μM. The IC50 value of BS-181 against CDK2/cycE is 880 nM. In a panel of cell lines representing a range of tumour types, including breast, lung, prostate and colorectal cancer, BS-181 inhibits cell growth with IC50 values ranging from 11.5 to 37 μM. BS-181 also promotes cell cycle arrest. BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after intraperitoneal administration of 10 mg/kg. BS-181 treatment (10 mg/kg) inhibits the growth of MCF-7 human xenografts in nude mice.[1]

Protocols

In vitro: BS-181 is dissolved in DMSO.[1]

References

[1] Ali S, et al. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009, 69(15): 6208-6215.

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