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PHA 767491 hydrochloride

Cat No. 3140

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Chemical Name: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyr idin-4-one hydrochloride

Biological Activity

Potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC₅₀ values are 10 and 34 nM respectively) that prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines (IC₅₀ ~ 0.86 - 5.87 μM) and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK-2) (IC₅₀ = 171 nM).

Technical Data

M.Wt:

249.7

Formula:

C₁₂H₁₁N₃O.HCl

Solubility:

Soluble to 100 mM in water and to 100 mM in DMSO

Purity:

>99 %

Storage:

Desiccate at RT

CAS No:

[845714-00-3]

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.

Resources

Certificate of Analysis / MSDS

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Material Safety Data Sheet: View current batch

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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.

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