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CCT-244747

Chemical Structure : CCT-244747

CAS No.: 1404095-34-6

CCT-244747 (CCT 244747;CCT244747)

Catalog No.: PC-45429Not For Human Use, Lab Use Only.

CCT-244747 (CCT244747) is a potent, highly selective, orally active, ATP competitive CHK1 inhibitor with biochemical IC50 of 8 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CCT-244747 (CCT244747) is a potent, highly selective, orally active, ATP competitive CHK1 inhibitor with biochemical IC50 of 8 nM.
CCT-244747 displays 75-fold selectivity against FLT3 and >1,000-fold selectivity against CHK2 and CDK1.
CCT-244747 inhibits cellular CHK1 activity (IC50=29-170nM), significantly enhances the cytotoxicity of several anticancer drugs and abrogates drug-induced S and G2 arrest in multiple tumor cell lines.
CCT-244747 enhances antitumor activity of gemcitabine and irinotecan in vivo.

Physicochemical Properties

M.Wt 408.457
Formula C20H24N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Pyrazinecarbonitrile, 3-[(1R)-2-(dimethylamino)-1-methylethoxy]-5-[[4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]amino]-

References

1. Walton MI, et al. Clin Cancer Res. 2012 Oct 15;18(20):5650-61.

2. Lainchbury M, et al. J Med Chem. 2012 Nov 26;55(22):10229-40.

3. Barker HE, et al. Mol Cancer Ther. 2016 Sep;15(9):2042-54.

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