ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors BS-181 hydrochloride

BS-181 hydrochloride

Product NameBS-181 hydrochloride
CAS1092443-52-1
MFC22H32N6
MW380.53
EINECS
MOL File1092443-52-1.mol

Chemical Properties

Density	1.16
storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Powder
pka	10.62±0.10(Predicted)
color	White to off-white

Usage And Synthesis

Uses

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

Definition

ChEBI: N5-(6-aminohexyl)-N7-(phenylmethyl)-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine is a pyrazolopyrimidine.

in vivo

BS-181 (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].

Animal Model:	7-week old female nu/nu-BALB/c athymic nude micewith MCF-7 cells^[1]
Dosage:	5 mg/kg or 10 mg/kg; 10 mg/kg or 20 mg/kg
Administration:	Intraperitoneal injection; twice daily or once total daily; 14 days
Result:	Inhibited tumor growth significantly.

IC 50

CDK7/CycH/MAT1: 0.021 μM (IC₅₀); CDK2/Cyc E: 0.88 μM (IC₅₀); CDK5/p35NCK: 3 μM (IC₅₀); CDK9/cycT: 4.2 μM (IC₅₀); CDK1/cycB: 8.1 μM (IC₅₀); CDK4/Cyc D1: 33 μM (IC₅₀); CDK6/cycD1: 47 μM (IC₅₀)

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. DOI:10.1158/0008-5472.CAN-09-0301
[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. DOI:10.2147/DDDT.S86317

BS-181 hydrochloride Supplier

BS-181 hydrochloride manufacturers

Related Product Information

Send Inquriy