Highly Selective CDK Inhibitors BS-181 Cas 1092443-52-1
Highly Selective CDK Inhibitors BS-181 Cas 1092443-52-1
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Chemical Information
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Product name:BS-181 |
Purity:98% min |
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CAS NO:1092443-52-1 |
Solubility:DMSO50 mg/mL (131.40 mM) |
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Molecular Formula:C22H33ClN6 |
Package:Package according to customer requirements |
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Molecular Weight:416.991 |
Storage:Store at -20℃ |
Quality control
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.
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