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CCT-245737 (PNT-737)
CCT-245737 (PNT-737) is an orally active, potent and selective CHK1 inhibitor, with an enzaymatic IC50 value of 1.4 nM against CHK1 enzyme, and exhibited >1,000-fold selectivity against CHK2 and CDK1. It potently inhibited cellular CHK1 activity (IC50 30-220nM) and enhanced gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. Mouse oral bioavailability was complete (100%) with extensive tumor exposure. Genotoxic-induced CHK1 activity (pS296 CHK1) and cell cycle arrest (pY15 CDK1) were inhibited both in vitro and in human tumor xenografts by CCT245737, causing increased DNA damage and apoptosis. CCT245737 uniquely enhanced gemcitabine antitumor activity to a greater degree than for higher doses of either agent alone, without increasing toxicity, indicating a true therapeutic advantage for this combination. Furthermore, development of a novel ELISA assay for pS296 CHK1 autophosphorylation, allowed the quantitative measurement of target inhibition in a RAS mutant human tumor xenograft of NSCLC at efficacious doses of CCT245737. Finally, CCT245737 also showed significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma (Ref. 1)
Catalog NO: CT-CCT245
Synonym: PNT737, CCT245737
CAS NO: 1489389-18-5
Mol. Formula: C16H16F3N7O∙1/4HCl
MW: 388.5
** in vivo Quality Material. >99% by achiral and chiral HPLCs. A recrystallized pale yellow crystalline powder (attached). Bulk stock!!! Prompt.