MRTX-1257 |
| Catalog No.GC64964 |
MRTX-1257 es un inhibidor de KRAS G12C selectivo, irreversible, covalente y activo por vÍa oral, con una IC50 de 900 pM para la fosforilaciÓn de ERK dependiente de KRAS en células H358.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2206736-04-9
Sample solution is provided at 25 µL, 10mM.
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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].
MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) shows rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice[1].MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups[1].MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained >70 days after cessation of treatment[1].
[1]. Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in Animal Models of Cancer.
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