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Cat. No.: HY-150639

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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.

For research use only. We do not sell to patients.

CAS No.: 2923700-82-5
Formula: C₂₀H₂₃ClFN₅O₂S₂
Molecular Weight:484.01

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

Everafenib Chemical Structure

CAS No.: 2923700-82-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

BRAF, MAPK^[1]

All Raf Isoforms :

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.

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).

Chemical Information

CAS No. 2923700-82-5
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kelly AM, et al. Target-Agnostic P-Glycoprotein Assessment Yields Strategies to Evade Efflux, Leading to a BRAF Inhibitor with Intracranial Efficacy. J Am Chem Soc. 2022 Jul 13;144(27):12367-12380. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Everafenib

High-Throughput Bioactive Compound Library

All Raf Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Everafenib Related Classifications

HY-150639 Related Classifications