118510

ATR Kinase Inhibitor II

• Synonym(s): ATR Kinase Inhibitor II, 3-Amino-6-(4-((1-(dimethylamino)propan-2-yl)sulfonyl)-phenyl)-N-phenylpyrazine-2-carboxamide
• Empirical Formula (Hill Notation): C₂₂H₂₅N₅O₃S
• Molecular Weight: 439.53
• UNSPSC Code: 12352200
• NACRES: NA.54

Properties

• assay: ≥97% (HPLC)
• Quality Level: 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

Description

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable