MRTX-1257
规格
| Cas Number | 2206736-04-9 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 5mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (176.76 mM); Ethanol: 30 mg/mL (53.03 mM); Water: Insoluble; |
| 简短描述 | Ras抑制剂 |
| 英文简短描述 | Ras Inhibitors |
| 过滤标签 | Ras,GPCR/G Protein,KRAS |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | MRTX-1257 是一种强效、选择性、不可逆、共价和口服活性的 KRAS G12C 抑制剂，对 H358 细胞中 KRAS 依赖性 ERK 磷酸化的 IC50 值为 900 pM。 |
| 英文描述 |
Information MRTX-1257 MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. Targets KRAS G12C ; KRAS dependent ERK phosphorylation (in H358 cells) ; 900 pM In vitro MRTX1257 demonstrates rapid, irreversible modification of GDP-bound recombinant KRAS G12C and suppresses ERK phosphorylation with an IC50 = 1 nM in the H358 cell line. In proteomics studies designed to assess global protein modification, MRTX1257 is shown to be highly selective for the targeted Cys12 of KRAS G12C versus other surface-exposed cysteine residues in NCI-H358 cells. In vivo MRTX1257 exhibits 31% bioavailability in mouse, demonstrates near-complete inhibition of KRAS signaling in tumor tissue, and complete durable tumor regression in MIA PaCa-2 xenografts. Cell Research(from reference) Cell lines：H358 Cells Concentrations：1 μM |