2. MAPK/ERK Pathway
  3. Raf
  4. 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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Everafenib Chemical Structure

Everafenib Chemical Structure

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Everafenib Related Antibodies

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Description

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[1].

IC50 & Target

BRAF, MAPK[1]
In Vitro

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.

Everafenib Related Antibodies

Western Blot Analysis[1]

Cell Line: A375 (V600EBRAF)
Concentration: 0.01, 0.1, 1 and 10 μM
Incubation Time: 1 or 24 h
Result: Inhibited phospho-ERK1/2 in a dose-dependent manner, also inhibited phospho-MEK1/2.
In Vivo

Everafenib (50 mg/kg; IP; once daily, for 5 days) increases median survival of melanoma mice from 39 to 50.5 days[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (intracranially injected with 5×104 A375 melanoma cells)[1]
Dosage: 50 mg/kg
Administration: IP; once daily, for 5 days
Result: Increased median survival from 39 to 50.5 days, and outperformed Dabrafenib (HY-14660).
Molecular Weight

484.01

Formula

C20H23ClFN5O2S2
SMILES

CC(C1=NC(C2=C(C(NS(CCC)(=O)=O)=CC(Cl)=C2)F)=C(C3=CC=NC(N)=N3)S1)(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Everafenib Related Classifications

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EverafenibRafRaf kinasesmetastatic melanomaBBBCNSV600E BRAFintracranialMAPK pathwayInhibitorinhibitorinhibit

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