1092443-52-1

Basic information

• Product Name: BS-181 hydrochloride
• Synonyms: BS-181 hydrochloride;BS 181;N5-(6-Aminohexyl)-3-isopropyl-N7-benzylpyrazolo[1,5-a]pyrimidine-5,7-diamine;BS-181 HCl
• CAS NO: 1092443-52-1
• Molecular Formula: C₂₂H₃₂N₆
• Molecular Weight: 380.52968
• Product Categories: Inhibitors
• Mol File: 1092443-52-1.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Density: 1.16
• Solubility: Soluble in DMSO
• CAS DataBase Reference: BS-181 hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: BS-181 hydrochloride(1092443-52-1)
• EPA Substance Registry System: BS-181 hydrochloride(1092443-52-1)

Safety Data

• Hazardous Substances Data: 1092443-52-1(Hazardous Substances Data)

Usage

General Description

BS-181 hydrochloride is a chemical compound that acts as a selective and potent inhibitor of the protein kinase WEE1, which plays a critical role in cell cycle regulation by controlling the G2/M checkpoint. By inhibiting WEE1, BS-181 hydrochloride can prevent the phosphorylation of CDK1 and delay the entry of cells into mitosis, ultimately leading to cell cycle arrest and potentially inducing apoptosis in cancer cells. BS-181 hydrochloride has shown promising anti-tumor activity in preclinical studies and may have potential for further development as a therapeutic agent for the treatment of various types of cancer.

Upstream product

• 1256288-44-4 tert-butyl benzyl(5-((6-((tert-butoxycarbonyl)amino)hexyl)amino)-3-isopropylpyrazolo[1,5-a]pyrimidin-7-yl)carbamate 

Relevant articles and documents

A novel pyrazolo[1,5- a ]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration

Cyclin-dependent protein kinases (CDKs) are central to the appropriate regulation of cell proliferation, apoptosis, and gene expression. Abnormalities in CDK activity and regulation are common features of cancer, making CDK family members attractive targets for the development of anticancer drugs. Here, we report the identification of a pyrazolo[1,5-a]pyrimidine derived compound, 4k (BS-194), as a selective and potent CDK inhibitor, which inhibits CDK2, CDK1, CDK5, CDK7, and CDK9 (IC50 = 3, 30, 30, 250, and 90 nmol/L, respectively). Cell-based studies showed inhibition of the phosphorylation of CDK substrates, Rb and the RNA polymerase II C-terminal domain, down-regulation of cyclins A, E, and D1, and cell cycle block in the S and G2/M phases. Consistent with these findings, 4k demonstrated potent antiproliferative activity in 60 cancer cell lines tested (mean GI50 = 280 nmol/L). Pharmacokinetic studies showed that 4k is orally bioavailable, with an elimination half-life of 178 min following oral dosing in mice. When administered at a concentration of 25 mg/kg orally, 4k inhibited human tumor xenografts and suppressed CDK substrate phosphorylation. These findings identify 4k as a novel, potent CDK selective inhibitor with potential for oral delivery in cancer patients.