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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.27%
- CAS No.: 3024878-19-8
- Formule: C36H39ClF4N8O3
- Masse moléculaire:743.19
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Stockage: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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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 inhibits both active and inactive KRASG12D-RAF1 RBD complex formation with single-digit nanomolar potency[1].
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.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3024878-19-8
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Appearance Solid
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Masse moléculaire 743.19
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (277 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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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Eras-4001 Related Classifications
HY-175870 Related Classifications
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