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MRTX1257

Development stage: Preclinical
Lead developer: Bristol Myers Squibb
Modality: Small Molecules
Administration: Oral

Overview

MRTX1257 is a potent, selective, covalent, and irreversible small-molecule inhibitor targeting KRAS with the G12C mutation. It is orally bioavailable and developed as an antineoplastic agent, particularly for KRAS G12C–mutant tumors, including non–small cell lung cancer (NSCLC). MRTX1257 inhibits KRAS-dependent ERK phosphorylation with an in vitro IC50 of 900 pM, demonstrating strong anti-tumor efficacy and radio-sensitizing potential in preclinical models. Treatment with MRTX1257 alters the tumor immune microenvironment towards a more pro-inflammatory, anti-tumor state and may synergize with immunotherapies and radiotherapy[1][2][3][5][7][9].

Other names: MRTX1257MRTX-1257MRTX 1257CAS 2206736-04-9CAS2206736-04-9CAS-2206736-04-9

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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