General description
A cell-permeable aminopyrazinyl-sulfone compound that acts as a potent, reversible and ATP-competitive inhibitor of ATR kinase (IC50 = 12 nM; Ki = 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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Charrier, J.D., et al. 2011. J. Med. Chem.54, 2320.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥97% (HPLC) |
| Quality Segment | 100 |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow |
| solubility | DMSO: 100 mg/mL |
| shipped in | wet ice |
| storage temp. | 2-8°C |
