Eras-4001
Based on 1 Customer Validation
Eras-4001 is a potent, orally active pan-KRAS inhibitor with Kd values of 110, 13 and 39 pM against wild-type, G12D and G12V mutant KRAS, respectively, and exhibits selectivity toward wild-type HRAS and NRAS. Eras-4001 inhibits ERK1/2 phosphorylation and cell viability in cancer cells. Eras-4001 induces tumor growth inhibition and regression in subcutaneous xenograft models. Eras-4001 can be used in research on non-small cell lung cancer, ovarian cancer, etc.
For research use only. We do not sell to patients.
- Purity : 99.30%
- CAS No.: 3024878-19-8
- 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
[1]|
K-Ras WT 110 pM (Kd) |
KRas G12D 13 pM (Kd) |
KRas G12V 39 pM (Kd) |
N-Ras 2460 nM (Kd) |
H-Ras 196 nM (Kd) |
ERK1 |
ERK2 |
In Vitro
Eras-4001 (3 hours) inhibits ERK phosphorylation in KRASWT and mutant cancer cell lines (AsPC-1, GP2d, MKN1, SW620, RKN, LoVo, LU99, A375), with quantified IC50 values reported[1].
Eras-4001 (4-7 days) potently inhibits 3D cell viability in KRASWT amplified cancer cell lines (IC50 0.7-9.1 nM), KRASG12X mutant cancer cell lines (IC50 0.7-56.0 nM), and KRASG13D mutant cancer cell lines (IC50 0.7-56.0 nM), and has minimal activity in KRASQ61H mutant and KRAS-independent cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Eras-4001 (30-300 mg/kg; p.o.; twice daily for 15 consecutive days) exhibits significant tumor regression in a mouse KRAS G12V ovarian cancer model[1].
Eras-4001 (30-100 mg/kg; p.o.; twice daily for 30 consecutive days) exhibits significant tumor regression in a patient-derived xenograft mouse model of G12D non-small cell lung cancer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tumor bearing mice[1]
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Dosage:10, 30, 100 and 300 mg/kg
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Administration:p.o.; twice daily for 20 days
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Result:Significantly induced tumor regression.
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Animal Model:Tumor bearing mice[1]
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Dosage:30, 100 and 300 mg/kg
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Administration:p.o.; twice daily for 15 days
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Result:Significantly induced tumor regression.
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Animal Model:Tumor bearing mice[1]
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Dosage:30 and 100 mg/kg
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Administration:p.o.; twice daily for 30 days
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Result:Significantly induced tumor regression.
- Western Blot
- Mammalian live/dead viability and cytotoxicity staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- How to Select the Route of Administration for Mammals
- Cell Cytotoxicity Assay
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3024878-19-8
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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 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.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (280 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 |
|---|---|---|---|---|---|
| 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 |
Eras-4001 Related Classifications
HY-175870 Related Classifications
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