Everafenib
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma.
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- No. CAS: 2923700-82-5
- Fòrmula: C20H23ClFN5O2S2
- Peso molecular:484.01
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
BRAF, MAPK[1]
Everafenib (1-10 μM; 1 or 24 h) inhibits MAPK signaling in A375 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 (V600EBRAF)
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Concentration:0.01, 0.1, 1 and 10 μM
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Incubation Time:1 or 24 h
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Result:Inhibited phospho-ERK1/2 in a dose-dependent manner, also inhibited phospho-MEK1/2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice (intracranially injected with 5×104 A375 melanoma cells)[1]
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Dosage:50 mg/kg
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Administration:IP; once daily, for 5 days
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Result:Increased median survival from 39 to 50.5 days, and outperformed Dabrafenib (HY-14660).
Chemical Information
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No. CAS 2923700-82-5
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Peso molecular 484.01
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Fòrmula C20H23ClFN5O2S2
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SMILES
CC(C1=NC(C2=C(C(NS(CCC)(=O)=O)=CC(Cl)=C2)F)=C(C3=CC=NC(N)=N3)S1)(C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Everafenib Related Classifications
HY-150639 Related Classifications
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