| Identification | Back Directory | [Name]
BS-181 hydrochloride | [CAS]
1092443-52-1 | [Synonyms]
CS-507
BS 181
CS-2137
BS-181 HCl
BS-181 free base
BS-181 hydrochloride
N5-(6-Aminohexyl)-3-isopropyl-N7-benzylpyrazolo[1,5-a]pyrimidine-5,7-diamine
Pyrazolo[1,5-a]pyrimidine-5,7-diamine, N5-(6-aminohexyl)-3-(1-methylethyl)-N7-(phenylmethyl)-
5-N-(6-aminohexyl)-7-N-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine,hydrochloride | [Molecular Formula]
C22H32N6 | [MDL Number]
MFCD22056527 | [MOL File]
1092443-52-1.mol | [Molecular Weight]
380.53 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 mice?with 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 |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
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www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
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