(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 KRAS^G12D-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].

ERAS-4001 (4-7 days) potently inhibits 3D cell viability in KRAS^G12C and KRAS^G13D mutant cancer cell lines with IC₅₀ values of 0.7-56.0 nM, but has minimal activity in KRAS-independent (A375, NCI-H226) and KRAS^Q61H mutant (NCI-H460) cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(7R)-Eras-4001 (100 mg/kg; p.o.; twice daily) delays tumor growth as monotherapy and enables complete tumor regression with durable immune memory when combined with anti-PD-1 in the KRAS^G12D PDAC syngeneic model^[1].
(7R)-Eras-4001 (50-150 mg/kg; p.o.; twice daily) reduces tumor growth as monotherapy and delivers enhanced antitumor efficacy when combined with cetuximab in the KRAS^G12D colorectal cancer CDX model^[1].
(7R)-Eras-4001 (30-300 mg/kg; p.o.; twice daily; 28 days) demonstrates a dose-dependent plasma exposure profile and inhibits tumor ERK1/2 signaling when administered orally BID for 28 days in the KRAS^G12D PDAC xenograft model^[1].
(7R)-Eras-4001 (100 mg/kg; p.o.; twice daily) delivers 77% to 83% tumor regression or growth inhibition in KRAS^G12D and KRAS^G12V mutant subcutaneous xenograft models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

743.19

C₃₆H₃₉ClF₄N₈O₃

3024878-21-2

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.