Gartisertib -d 8 (VX-803-d 8 ) is the deuterium labeled Gartisertib. Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a K i of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 ( Chk1 ) phosphorylation with an IC50 of 8 nM. Antitumor activity [1] [2].
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
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.
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
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.