217707

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

• Synonym(e): Cdc7/Cdk9 Inhibitor - CAS 845714-00-3 - Calbiochem, 2-(Pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridinone, PHA-767491, Chk2 Inhibitor VI
• Empirische Formel (Hill-System): C₁₂H₁₁N₃O
• CAS-Nummer: 845714-00-3
• Molekulargewicht: 213.24
• UNSPSC Code: 12352200

Eigenschaften

• assay: ≥90% (HPLC)
• Quality Segment: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: pink
• solubility: DMSO: 25 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Beschreibung

General description

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.

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 10-13 - German Storage Class 10 to 13