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217201 ATR Kinase Inhibitor II (3-Amino-6-(4-((1-(dimethylamino)propan-2-yl)sulfonyl)-phenyl)-N-phenylpyrazine-2-carboxamide) CAS:

Specifications
References
Grade
Highly Purified
Molecular Formula
C₂₂H₂₅N₅O₃S
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
4°C

A cell-permeable aminopyrazinyl-sulfone compound that acts as a potent, reversible and ATP-competitive inhibitor of ATR kinase (IC50 = 12nM; Ki = 6nM) with excellent selectivity over ATM, DNA-PK (IC50 > 8uM) and in a 50-kinase panel (% inhibition at 2uM = 59, 57, 55, 52, 43 and 42 for AMPK, Lck, RIPK2, Ret, IKK-alpha and FGFR3, respectively). Shown to block pH2AX-Ser139 (IC50 = 420nM in hydroxyurea treated HT29 cells) and preferentially enhance cisplatin cytotoxicity against tumor cells over normal cells by ~7-fold at 620nM.

Molecular Formula
C₂₂H₂₅N₅O₃S
Solubility
DMSO
Storage and Stability
May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Purity
~97% (HPLC)
Form
Supplied as a yellow powder.
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.
References
1. Charrier, J.D., et al. 2011. J. Med. Chem. 54, 2320.
USBio References
No references available
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