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VER-158411

Chemical Structure : VER-158411

CAS No.: 1174664-88-0

VER-158411 (VER-00158411;V-158411)

Catalog No.: PC-60279Not For Human Use, Lab Use Only.

A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively; dispalys >1,000-fold selectivity over CDK1; reduces pChk1 (S296) and pChk2 (S516) levels in a concentration dependent fashion in cells treated with etoposide with IC50s of 48 nM for Chk1 and 904 nM for Chk2; potentiates the cytotoxicity of chemotherapeutic agents in a variety of p53 deficient human tumor cell lines (GI50=0.5-9.5 uM) and human colon tumor xenograft models.

Physicochemical Properties

M.Wt 538.652
Formula C31H34N6O3
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

1-benzyl-N-(5-(5-(3-(dimethylamino)-2,2-dimethylpropoxy)-1H-indol-2-yl)-6-oxo-1,6-dihydropyridin-3-yl)-1H-pyrazole-4-carboxamide

References

1. Massey AJ, et al. Oncotarget. 2015 Nov 3;6(34):35797-812.

2. Alsubhi N, et al. Mol Oncol. 2016 Feb;10(2):213-23.

3. Wayne J, et al. Oncotarget. 2016 Dec 20;7(51):85033-85048.

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