MRTX1133
Cat. No.：YN322437
| 产品名称: | MRTX1133 |
| CAS No.: | 2621928-55-8 |
| Chemical Name: | 4-[4-(3,8-diazabicyclo[3.2.1]oct-3-yl)-8-fluoro-2-[[(2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoro-2-naphthalenol |
| Synonyms: | |
| 分子量: | 600.6336896 |
| 分子式: | C33H31F3N6O2 |
| SMILES: | FC1=C(C2=CC(O)=CC3=C2C(C#C)=C(F)C=C3)N=CC4=C1N=C(N=C4N5CC6NC(CC6)C5)OC[C@]78N(CCC8)C[C@H](C7)F |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | MRTX1133 是一种非共价、强效和选择性KRAS G12D抑制剂。MRTX1133 以最佳方式填充开关 II 口袋，并延伸三个取代基以与蛋白质良好地相互作用，对 KRAS G12D 的KD为 0.2 pM。MRTX1133 阻止 SOS1 催化的核苷酸交换和/或KRAS G12D/GTP/RAF1 复合物的形成，从而抑制突变体 KRAS 依赖性信号转导。MRTX1133 选择性抑制 KRAS G12D 突变体肿瘤细胞，但不抑制 KRAS 野生型细胞。MRTX1133 在细胞实验中具有一位数纳摩尔活性， |
| IC50和靶点: | [{name:"KRas G12D:0.2 pM (Kd)"}] |
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| Clinical Trial: | |
| Solvent & Solubility: |
Swiatnicki, M., Engel, L., Shrestha, R., et al.Profiling oncogenic KRAS mutant drugs with a cell-based Lumit p-ERK immunoassaySLAS Discov.S2472-5552(22),(2022)
