| Description |
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity[1][2].
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| Related Catalog |
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| Target |
ATR:<150 pM (Ki)
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| In Vivo |
In monotherapy efficacy studies ATR inhibitor 2 (VX-970, M6620) shows tumor stasis to regression in tumor models with alternative lengthening of telomeres (ALT). In combination with PARP inhibitors, tumor regression could be observed in triple-negative breast cancer xenograft models[1].
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| References |
[1]. Frank T. Zenke, et al. Abstract 369: Antitumor activity of M4344, a potent and selective ATR inhibitor, in monotherapy and combination therapy. Experimental and Molecular Therapeutics. [2]. Gorecki L, et al. Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy. Pharmacol Ther. 2020 Feb 26:107518.
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