MU380

MU380 is a **potent and selective checkpoint kinase 1 (CHK1) inhibitor** developed as a small molecule analog of SCH900776 (MK8776), featuring a metabolically robust N-trifluoromethylpyrazole moiety that confers resistance to oxidative N-dealkylation and improved metabolic stability. MU380 induces apoptosis, impairs cell cycle progression, and exhibits significant single-agent activity particularly in **chronic lymphocytic leukemia** and **docetaxel-resistant prostate cancer** models, including those with TP53 and ATM mutations. It has demonstrated ability to sensitize various cancer cell lines to DNA antimetabolites—especially gemcitabine—and enhances chemotherapy-induced DNA damage, leading to cell death via mitotic catastrophe. Preclinical studies support its activity in both in vitro and in vivo (xenograft) models, including potent effects in TP53-mutant settings and tumor growth suppression in mouse models[1][2][3][6][9].

Other names

(R)-6-bromo-5-(piperidin-3-yl)-3-(1-(trifluoromethyl)-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-7-amine6-Bromo-5-(3R)-3-piperidinyl-3-[1-(trifluoromethyl)-1H-pyrazol-4-yl]-pyrazolo[1,5-a]pyrimidin-7-amine