MRTX-1257 是选择性的、不可逆的、共价的并具有口服活性的 KRAS G12C 抑制剂，其在 H358 细胞中测得 KRAS 依赖 ERK 磷酸化的 IC50 值为 900 pM。
货号:ajcx38646
CAS:2206736-04-9
分子式:C33H39N7O2
分子量：565.71
溶解度:DMSO : 55 mg/mL (97.22 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.