MRTX-1257 |
| Catalog No.GC64964 |
MRTX-1257은 H358 세포에서 KRAS 의존적 ERK 인산화에 대한 IC50이 900pM인 선택적, 비가역적, 공유 결합 및 경구 활성 KRAS G12C 억제제입니다.
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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