217707
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 Segment
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
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.
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)
Storage Class
10-13 - German Storage Class 10 to 13
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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