BS-181

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Chemical Information

Product name：BS-181	Purity：98% min
CAS NO：1092443-52-1	Solubility：DMSO : ≥ 50 mg/mL (131.40 mM)
Molecular Formula：C₂₂H₃₃ClN₆	Package：Package according to customer requirements
Molecular Weight：416.991	Storage：Store at -20℃

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Remarks

BS-181 is a highly selective CDK inhibitor for CDK7 with an IC(50) of 21 nmol/L. Testing of other CDKs as well as another 69 kinases showed that BS-181 only inhibited CDK2 at concentrations lower than 1 micromol/L, with CDK2 being inhibited 35-fold less potently (IC(50) 880 nmol/L) than CDK7. In MCF-7 cells, BS-181 inhibited the phosphorylation of CDK7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines, and showed antitumor effects in vivo.

Related Products:

BMS-265246; LDC000067; Ribociclib; SU9516; Purvalanol A; Alvocidib; AZD-5597; Kenpaullone; ON123300; JSH-150; Riviciclib

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]. 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.