VX-803 (M4344)

Names

[ Name ]:
VX-803 (M4344)

[Synonym ]:
MFCD31803930

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₉F₂N₉O₃

[ Molecular Weight ]:
541.55

[ Storage condition ]:
-20°C

Related Compounds

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