Cdc7/Cdk9 Inhibitor - CAS 845714-00-3 - Calbiochem

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-3β, 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.

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-3β, 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.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)