3024878-21-2
Chemical Structure
(7R)-Eras-4001
- CAS No.: 3024878-21-2
- Formula:C36H39ClF4N8O3
- Molecular Weight:743.19
InChIKey: MQIGGDZYPCCUDF-IJAHGLKVSA-N
SMILES: FC1=C([C@H]2CC(N=C(OC[C@@]34CCCN3CC(C4)=C)N=C5N6CC7=C(Cl)C(C(N(C)C)=O)=NN7CCC6)=C5CO2)C(C(F)(F)F)=C(C#CC)C=C1N
Biological Activity: (7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRASG12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer[1][2].
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(7R)-Eras-4001 | (7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRASG12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer. | |||||||||||||||||||||
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- [1]. Bae J H, Lin B, Lew E D, et al. ERAS-4001 is a pan-KRAS inhibitor with robust anti-tumor activity in KRAS altered solid tumors[J]. ERAS, 2025, 4001(5.65): 1.65.
- [2]. Zhang Y, et al. Heterocyclic substituted pyrimidopyran derivative, its preparation method and application for treating pan-KRAS related diseases. World Intellectual Property Organization, WO2023246914 A1. 2023-12-28.
Keywords
