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BS-181 CAS: 1092443-52-1

Category: Inhibitors
Product Name: BS-181
Cat No: I000382
CAS No: 1092443-52-1
Synonyms: 5-N-(6-aminohexyl)-7-N-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine
Molecular Formula: C22H32N6
Molecular Weight: 380.53
Solubility: DMSO ≥80mg/mL Water ≥2.8mg/mL Ethanol ≥9mg/mL
Target: Cyclin-Dependent Kinases
IC50: 21 nM
Storage: Store at -20°C
CAS 1092443-52-1,BS-181
  • Description

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
IC50 Value: 21 nM
Target: CDK7
in vitro: BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 μM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 μM, and only shows inhibition for several kinases from other classes at high concentrations (>10 μM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 μM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.
in vivo: BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity.

  • 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.
[2]. Lü XC, Montelius-Alatalo K, Helou K, Klinga-Levan K, Islam Q, Levan G, R?hme D. SourceDepartment of Genetics, Lundberg Laboratory, G?teborg University, Sweden.Isolation of DNA markers for the rat Sai 1 gene for suppression of anchorage independence by using representational difference analysis.Somat Cell Mol Genet. 1997 Jan;23(1):63-74.
[3]. Islam MQ, Szpirer J, Szpirer C, Islam K, Dasnoy JF, Levan G.A gene for the suppression of anchorage independence is located in rat chromosome 5 bands q22-23, and the rat alpha-interferon locus maps at the same region.J Cell Sci. 1989 Feb;92 ( Pt 2):147-62.

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