2639608-44-7
Chemical Structure
MRTX-1257-d6
- CAS No.: 2639608-44-7
- Formula:C33H33D6N7O2
- Molecular Weight:571.75
IUPAC Name: 2-((S)-1-acryloyl-4-(7-(8-(methyl-d3)naphthalen-1-yl)-2-(((S)-1-(methyl-d3)pyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile
InChIKey: YRYQLVCTQFBRLD-FGLOIYPXSA-N
SMILES: [2H]C([2H])([2H])N(CCC1)[C@@H]1COC2=NC(N3C[C@@H](N(CC3)C(C=C)=O)CC#N)=C4C(CN(C5=CC=CC6=C5C(C([2H])([2H])[2H])=CC=C6)CC4)=N2
Biological Activity: MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1][2].
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MRTX-1257-d6 | MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. | |||||||||||||||||||||
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MRTX-1257 | 99.71% | MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. | ||||||||||||||||||||
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- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-220. [Content Brief]
- [2]. Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in Animal Models of Cancer.
Keywords
