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Merck
CN

118510

ATR Kinase Inhibitor II

别名:

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

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关于此项目

经验公式(希尔记法):
C22H25N5O3S
分子量:
439.53
NACRES:
NA.54
UNSPSC Code:
12352200
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assay

≥97% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: 100 mg/mL

shipped in

wet ice

Quality Level

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)

存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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