VE 821 New
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.
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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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