BS-181 dihydrochloride 

BS-181 dihydrochloride 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 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC₅₀=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy^[1][2].

BS-181 dihydrochloride (0-40 μM; 72 hours) inhibits cancer cells growth, it is against Breast cancer cell lines growth with IC₅₀ values ranging from 15.1 μM to 20 μM, it is against Colorectal cancer cell lines growth with IC₅₀ values ranging from 11.5 μM to15.3 μM and is against lung, osteosarcoma, prostate and liver cancer cell lines with IC₅₀ values ranging from 11.5 μM to 37.3 μM, respectively^[1].
BS-181 dihydrochloride (0-50 μM; 4 hours) shows inhibition of phosphorylation of the RNA polymerase II C-terminal domain (CTD) at serine 5 (P-Ser5). It down-regulates CDK4 and cyclin D1 expression while does not effect other CDKs and cyclins^[1].
BS-181 dihydrochloride (0-50 μM; 24 hours) shows an increase in cells in G1, accompanied by a reduction in cell numbers in S and G2/M at low concentrations. At higher concentrations, however, cells accumulates in the sub-G1, indicative of apoptosis^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BS-181 dihydrochloride (intraperitoneal injection; 10 mg/kg, 20 mg/kg; single dose) is well tolerated in mice without apparent weight altering^[1].
BS-181 dihydrochloride (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

453.45

C₂₂H₃₄Cl₂N₆

1883548-83-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]