General description

A cell-permeable aminopyrazinyl-sulfone compound that acts as a potent, reversible and ATP-competitive inhibitor of ATR kinase (IC₅₀ = 12 nM; K_i = 6 nM) with excellent selectivity over ATM, DNA-PK (IC₅₀ >8 µM) and in a 50-kinase panel (% inhibition at 2 µM = 59, 57, 55, 52, 43 and 42 for AMPK, Lck, RIPK2, Ret, IKKα and FGFR3, respectively). Shown to block pH2AX-Ser¹³⁹ (IC₅₀ = 420 nM in hydroxyurea treated HT29 cells) and preferentially enhance cisplatin (Cat. No. 232120) cytotoxicity against tumor cells over normal cells by ~7-fold at 620 nM.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Charrier, J.D., et al. 2011. J. Med. Chem.54, 2320.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)