PHA-767491 HCl

  • Chemical Properties
CAS No. 942425-68-5 Cat. No. BCP28863
Name PHA-767491 HCl
Synonyms PHA 767491 Hydrochloride; PHA 767491 HCl ; PHA767491 HCl ;PHA767491; PHA-767491; PHA 767491; CAY10572; CAY-10572; CAY 10572;
Formula C12H12ClN3O M. Wt 249.7
  • Biological Activity
Description PHA-767491, also known as CAY10572, is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. PHA-767491 in combination with 5-FU exhibited much stronger cytotoxicity and induced significant apoptosis manifested by remarkably increased caspase 3 activation and poly(ADP-Ribose) polymerase fragmentation in HCC cells. PHA-767491 directly counteracted the 5-FU-induced phosphorylation of Chk1, a substrate of Cdc7; and decreased the expression of the anti-apoptotic protein myeloid leukemia cell 1, a downstream target of Cdk9.
Pathways Cell Cycle/DNA Damage 
Targets CDK 

Structure

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