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Axon 3733
CAS [2206736-04-9]
MF C33H39N7O2MW 565.71
MRTX1257 is an orally available, potent, selective, and irreversible covalent inhibitor of KRAS G12C. It inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 0.9 nM, and is highly selective for the Cys12 of KRAS G12C in NCI-H358 cells over other cysteines; Demonstrates robust target engagement in vivo; Exhibits rapid and sustained efficacy against MIA PaCa-2 Xenocrafts, in which, at 100 mg/kg daily dose, leads to complete responses that are maintained >70 days after cessation of treatment.
KEYWORDS: MRTX1257 | Supplier | KRAS-G12C inhibitor | MRTX-1257 | MRTX 1257 | CT-MRTX1257 | CAS [2206736-04-9] | GTP | KRAS | Inhibitor | Enzymes
2-((S)-1-acryloyl-4-(7-(8-methylnaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile
[2206736-04-9]
The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.
Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!
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