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.
Cat.No
DC75825
Name
PHA-767491 HCl
Chemical Properties
CAS
942425-68-5
Formula
C12H12CLN3O
MW
249.7
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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