ATR Kinase Inhibitor II

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.

Packaged under inert gas

Toxicity: Standard Handling (A)

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

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

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