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Eras-4001是一种小分子泛KRAS抑制剂,能够同时作用于KRAS野生型及多种突变形式,并抑制其与RAF等效应蛋白的信号传导,从而阻断RAS/MAPK通路活性。Eras-4001在前期研究中表现出对KRAS的高亲和力(纳摩尔级IC₅₀),并在多种KRAS突变肿瘤模型中诱导肿瘤回缩,显示出潜在的抗肿瘤治疗价值。
Eras-4001是一种小分子泛KRAS抑制剂,能够同时作用于KRAS野生型及多种突变形式,并抑制其与RAF等效应蛋白的信号传导,从而阻断RAS/MAPK通路活性。Eras-4001在前期研究中表现出对KRAS的高亲和力(纳摩尔级IC₅₀),并在多种KRAS突变肿瘤模型中诱导肿瘤回缩,显示出潜在的抗肿瘤治疗价值。


| 产品描述 | Eras-4001 is a small-molecule pan-KRAS inhibitor capable of targeting both wild-type KRAS and various mutant forms simultaneously. Eras-4001 inhibits signaling between KRAS and effector proteins such as RAF, thereby blocking the activity of the RAS/MAPK pathway. In preliminary studies, this compound has demonstrated high affinity for KRAS (nano-molar IC₅₀) and induced tumor regression in multiple KRAS-mutant tumor models, indicating potential value for antitumor therapy. |
| 靶点活性 | H727 cells:3.51 nM, AsPC1 cells:1.78 nM, MKN1 cells:3.6 nM, SW620 cells:12.6 nM, LU99 cells:2.7 nM |
| 体内活性 | Eras-4001(150 mg/kg,PO,BID)给药28天后肿瘤体积抑制率达97.2%,对人体结肠癌GP2D小鼠异种移植瘤有显著抑制作用。 |
| 分子量 | 743.19 |
| 分子式 | C36H39ClF4N8O3 |
| CAS No. | 3024878-19-8 |
| Smiles | C(OC1=NC(=C2C(=N1)C[C@H](OC2)C3=C(C(F)(F)F)C(C#CC)=CC(N)=C3F)N4CC=5N(CCC4)N=C(C(N(C)C)=O)C5Cl)[C@@]67N(CC(=C)C6)CCC7 |
| 密度 | no data available |
| 存储 |
对于不同动物的给药剂量换算,您也可以参考 更多