Everafenib

CAT: 0804-HY-150639Size: 1 EachDry Ice: NoHazardous: No

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CAT#:0804-HY-150639Size:1 Each

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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 and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma[1].

CAS Number

2923700-82-5

UNSPSC

12352005

Target

Raf

Type

Reference compound

Related Pathways

MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/everafenib.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C20H23ClFN5O2S2

Molecular Weight

484.01

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

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