1613191-99-3

1613191-99-3 structure

Name: VX-803 (M4344)
Chemical Name: ATR inhibitor 2
CAS Number: 1613191-99-3
Molecular Formula: C₂₅H₂₉F₂N₉O₃
Molecular Weight: 541.55
Catalog: Signaling Pathways Cell Cycle/DNA Damage ATM/ATR
Create Date: 2020-06-01 16:04:01
Modify Date: 2024-01-12 08:04:26
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].

Name	ATR inhibitor 2
Synonyms	MFCD31803930

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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> ATM/ATR Signaling Pathways >> PI3K/Akt/mTOR >> ATM/ATR
Target	ATR:<150 pM (Ki)
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].
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.