MRTX849 是一种可口服、突变选择性的KRas G12C共价抑制剂，具有潜在抗肿瘤活性。它在半胱氨酸 12 残基处与 KRas G12C 共价结合，将蛋白锁定在非活性的 GDP 结合构象中，抑制 KRas 依赖性信号转导。

MRTX849 is a potent, selective and covalent KRASG12C inhibitor with potential antineoplastic activity. It selectively modifies mutant cysteine 12 in GDP-bound KRASG12C, and inhibits KRAS-dependent signaling.

MRTX849 demonstrated pronounced tumor regression in 17 of 26 (65%) KRASG12C-positive cell line- and patient-derived xenograft models from multiple tumor types, and objective responses have been observed in patients with KRASG12C-positive lung and colon adenocarcinomas[1].

2326521-71-3

C32H35ClFN7O2

604.13

MRTX849

DMSO:100 mg/mL (165.53 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years