(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.
For research use only. We do not sell to patients.
- CAS No.: 3024878-21-2
- Formula: C36H39ClF4N8O3
- Molecular Weight:743.19
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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KRAS(G12C) |
KRas G12D |
KRas G12V |
ERAS-4001 (4-7 days) potently inhibits 3D cell viability in KRASG12C and KRASG13D mutant cancer cell lines with IC50 values of 0.7-56.0 nM, but has minimal activity in KRAS-independent (A375, NCI-H226) and KRASQ61H mutant (NCI-H460) cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620, LU99 and MKN-1
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Concentration:IC50
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Incubation Time:/
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Result:Inhibited cell viability with IC50s of 12.6 nM, 3.6 nM and 2.7 nM, respectively.
(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 KRASG12D 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 KRASG12D PDAC xenograft model[1].
(7R)-Eras-4001 (100 mg/kg; p.o.; twice daily) delivers 77% to 83% tumor regression or growth inhibition in KRASG12D and KRASG12V mutant subcutaneous xenograft models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pancreatic ductal adenocarcinoma tumor-bearing Mice[1]
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Dosage:100 mg/kg
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Administration:p.o.; twice daily
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Result:Delayed tumor growth relative to vehicle as monotherapy.
Enabled complete tumor regression with durable immune memory when combined with anti-PD-1, with all mice having no measurable tumors from day 50 through study end and no tumors forming after KPC cell rechallenge.
Chemical Information
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CAS No. 3024878-21-2
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Appearance Solid
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Molecular Weight 743.19
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Formula C36H39ClF4N8O3
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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