化合物MRTX-1257 T16143

Product Introduction
Bioactivity


英文名: MRTX-1257

描述: MRTX-1257 是选择性的、可口服的不可逆共价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。

体内活性: MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups. MRTX-1257 dosed of 100 mg/kg daily causes complete responses that are maintained >70 days after cessation of treatment. MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) displays rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice .

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 54 mg/mL(95.46 mM)


关键字: Inhibitor | selective | inhibit | Ras | G12C | irreversible | ERK | phosphorylation | H358 cells | cancer | mutant | MRTX1257 | covalent | MRTX 1257 | KRAS | MRTX-1257

相关产品: Deltarasin | Kobe0065 | NSC 23766 trihydrochloride | SOS1/KRAS-IN-1 | Rhosin hydrochloride | CCG-222740 | Y16 | Salirasib | APS6-45 | KRAS G12C inhibitor 15

相关库: Anti-Cancer Metabolism Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | GPCR Compound Library | Anti-Colorectal Cancer Compound Library | Reprogramming Compound Library | NO PAINS Compound Library | Covalent Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途