MRTX-1257 |
| Catalog No.GC64964 |
MRTX-1257 est un inhibiteur sélectif, irréversible, covalent et oral de KRAS G12C, avec une IC50 de 900 pM pour la phosphorylation de ERK dépendante de KRAS dans les cellules H358.
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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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