Chemical Name: 3-Amino-6-[4-(methlsulfonyl)phenyl)-N-phenyl-2-pyrazinecarboxamide
Biological ActivityHigh affinity and selective ATP-competitive ATR inhibitor (Ki = 13 nM). Exhibits >75-fold selectivity for ATR over related kinases mTOR, DNA-PK, PI 3-Kγ and PIKKs (Ki values are >1, 2.2, 3.9 and 16 μM, respectively) and a panel of other kinases. Induces cell death in colon cancer cell lines in vitro and sensitizes tumor cells to treatment with DNA damaging anticancer agents.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR.
Reaper et al.
ATR inhibitors as a synthetic lethal therapy for tumours deficient in ARID1A.
Williamson et al.
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