(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.
- Purity : 97.02%
- 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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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KRAS(G12C) |
KRas G12D |
KRas G12V |
In Vitro
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.
In Vivo
(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.
- Kinase activity and phosphorylation assays
- Western Blot
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Kinase activity and phosphorylation assays
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
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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Color White to off-white
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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
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (134.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.3456 mL | 6.7278 mL | 13.4555 mL | 33.6388 mL |
| 5 mM | 0.2691 mL | 1.3456 mL | 2.6911 mL | 6.7278 mL | |
| 10 mM | 0.1346 mL | 0.6728 mL | 1.3456 mL | 3.3639 mL | |
| 15 mM | 0.0897 mL | 0.4485 mL | 0.8970 mL | 2.2426 mL | |
| 20 mM | 0.0673 mL | 0.3364 mL | 0.6728 mL | 1.6819 mL | |
| 25 mM | 0.0538 mL | 0.2691 mL | 0.5382 mL | 1.3456 mL | |
| 30 mM | 0.0449 mL | 0.2243 mL | 0.4485 mL | 1.1213 mL | |
| 40 mM | 0.0336 mL | 0.1682 mL | 0.3364 mL | 0.8410 mL | |
| 50 mM | 0.0269 mL | 0.1346 mL | 0.2691 mL | 0.6728 mL | |
| 60 mM | 0.0224 mL | 0.1121 mL | 0.2243 mL | 0.5606 mL | |
| 80 mM | 0.0168 mL | 0.0841 mL | 0.1682 mL | 0.4205 mL | |
| 100 mM | 0.0135 mL | 0.0673 mL | 0.1346 mL | 0.3364 mL |
(7R)-Eras-4001 Related Classifications
HY-175870A Related Classifications
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