PHA-767491
2-(Pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridinone Pink solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable pyrrolopyridinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of Cdc7 and Cdk9 (IC50 = 10 and 34 nM, respectively) with good selectivity over a panel of 31 other kinases, including GSK-3b, Cdk2, Cdk1, Cdk5, MK-2, Plk1, and Chk2 (IC50 = 0.22, 0.24, 0.25, 0.46, 0.47, 0.98, and 1.1 µM, respectively). Cellular treatment of PHA76749 results in a prevention of the activation of DNA replication origins without the inhibition of replication fork progression. Shown to inhibit the proliferation of 61 cell lines in vitro (IC50 ≤10 µM) and exhibit antitumor activity in both mice and rats in vivo. Purity: ≥90% by HPLC. Ref.: Montagnoli, A., et al. 2008. Nat Chem Biol. 4, 357. Vanotti, E., et al. 2008. J. Med. Chem. 51, 487. Anderson, D.R., et al. 2007. J. Med. Chem. 50, 2647. |
