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217707

Sigma-Aldrich

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

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C12H11N3O
CAS Number:
Molecular Weight:
213.24
UNSPSC Code:
12352200

assay

≥90% (HPLC)

Quality Level

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

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Storage Class

10-13 - German Storage Class 10 to 13


Certificates of Analysis (COA)

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