PHA 767491 hydrochlorideA potent, ATP-competitive dual cdc7/cdk9 inhibitor

PHA 767491 hydrochloride (CAS 942425-68-5)

PHA 767491 hydrochloride | CAS 942425-68-5 is rated 5.0 out of 5 by 2.
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Application: A potent, ATP-competitive dual cdc7/cdk9 inhibitor
CAS Number: 942425-68-5
Purity: >99%
Molecular Weight: 249.7
Molecular Formula: C12H11N3O•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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PHA 767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. PHA 767491 hydrochloride induces apoptosis in a p53-independent manner, and inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 μM). The compound also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK-2) (IC50 = 171 nM).


References

Anderson et al (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) J.Med.Chem. 50 2647. Jackson (2008) Stopping replication, at the beginning. Nature Chem.Biol. 4 331. Montagnoli et al (2008) A cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumour activity. Nature Chem.Biol. 4 357.

Physical State :
Solid
Solubility :
Soluble to 100 mM in Water and to 100 mM in DMSO
Storage :
Desiccate at room temperature
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11715766
SMILES :
C1CNC(=O)C2=C1NC(=C2)C3=CC=NC=C3.Cl

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Certificate of Analysis

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PHA 767491 hydrochloride  Product Citations

See how others have used PHA 767491 hydrochloride. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 28630312  2017. Proc. Natl. Acad. Sci. U.S.A. 114: E5352-E5361.

PMID: # 27587400  Xu, X. et al. 2016. J. Biol. Chem. 291: 22544-22558.

PMID: # 25737283  Sansam, CG. et al. 2015. Genes Dev. 29: 555-66.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from PHA 767491 hydrochloride has been known to PHA 767491 hydrochloride has been known to block DNA replication and induce apoptosis in a p53 independent manner (in vivo). It also inhibits cell proliferation in a variety of human cell lines. -SCBT QC
Date published: 2015-02-24
Rated 5 out of 5 by from An increase in cleaved PARP An increase in cleaved PARP-1 protein was observed by WB in Jurkat cells post treatment with PHA 767491 hydrochloride. -SCBT QC
Date published: 2015-02-19
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