MRTX1257

Based on 3 reference(s) in Google Scholar 8 10 3

Axon 3733

CAS [2206736-04-9]

MF C33H39N7O2
MW 565.71

  • Purity: 99%
  • Optical purity: 99% d.e.
  • Soluble in DMSO
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MRTX1257

Description

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.

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KEYWORDS: MRTX1257 | Supplier | KRAS-G12C inhibitor | MRTX-1257 | MRTX 1257 | CT-MRTX1257 | CAS [2206736-04-9] | GTP | KRAS | Inhibitor | Enzymes

Irreversible covalent inhibitor of KRAS G12C

Chemical name

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

Source information

Sold in collaboration with Chemietek

Parent CAS No.

[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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