1792214-00-6
Chemical Structure
Gartisertib-d8
Synonym(s): VX-803-d8; M4344-d8; ATR inhibitor 2-d8
- CAS No.: 1792214-00-6
- Formula:C25H21D8F2N9O3
- Molecular Weight:549.60
InChIKey: QAYHKBLKSXWOEO-YEBVBAJPSA-N
SMILES: O=C(C1=C2N=CC(F)=CN2N=C1N)NC3=C(N4CCC(C(N5C([2H])([2H])C([2H])([2H])N(C6COC6)C([2H])([2H])C5([2H])[2H])=O)CC4)C(F)=CN=C3
Biological Activity: Gartisertib-d8 (VX-803-d8) is the deuterium labeled Gartisertib (HY-136270). Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity[1][2].
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Gartisertib-d8 | Gartisertib-d8 (VX-803-d8) is the deuterium labeled Gartisertib (HY-136270). Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity. | |||||||||||||||||||||
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Gartisertib | 99.77% | Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity. | ||||||||||||||||||||
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- [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. [Content Brief]
Keywords
