Key Spec Table
|Empirical Formula||CAS #|
Pricing & Availability
An invalid quantity was specified. The product quantity has been adjusted.
|5049720001||Glass bottle||10 mg||
|Overview||A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13 nM; IC50/[ATP] = 70 nM/50 µM and 128 nM/100 µM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1 µM, respectively, against DNA-PK, PI 3-Kγ, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10 µM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24 h) VE-821 treatment, either alone or in synergy with Cisplatin (Cat. No. 232120), results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥72 h) in cultures with ATM-p53 pathway defects.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
|Synonyms||VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV|
|References||Prevo, R., et al. 2012, Cancer Biol. Ther. 13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer 107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7, 428.|
|Structure formula Image|
|Primary Target K<sub>i</sub>||13nM|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Prevo, R., et al. 2012, Cancer Biol. Ther. 13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer 107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7, 428.|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.