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217200 ATR Inhibitor IV (VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV) CAS: 1232410-49-10

Specifications
References
CAS Number
1232410-49-10
Grade
Highly Purified
Molecular Formula
C18H16N4O3S
Molecular Weight
368.41
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
-20°C

A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13nM; IC50/[ATP] = 70nM/50uM and 128nM/100uM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1uM, respectively, against DNA-PK, PI 3-K-gamma, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10uM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24h) VE-821 treatment, either alone or in synergy with Cisplatin, 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 (≥72h) in cultures with ATM-p53 pathway defects.

Synonyms
VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV
CAS No
1232410-49-10
Molecular Formula
C₁₈H₁₆N₄O₃S
Solubility
As Reported
Primary Target
ATR
Primary Target Ki
13nM
Molar Mass
368.41
Appearance
Yellow solid
Purity
≥98% (HPLC)
Storage and Stability
May be stored at 4°C. For long-term storage store at -20°C. Stable for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Store under inert gas. Light sensitive.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards
 All products should be handled by qualified personnel only, trained in laboratory procedures.
References
1. Prevo, R., et al. 2012, Cancer Biol. Ther. 13:1072; 2. Pires, I.M., et al. 2012, Br. J. Cancer 107:291; 3. Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7:428
USBio References
No references available
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