2923700-82-5
Chemical Structure
Everafenib
- CAS No.: 2923700-82-5
- Formula:C20H23ClFN5O2S2
- Molecular Weight:484.01
IUPAC Name: N-(3-(5-(2-aminopyrimidin-4-yl)-2-(tert-butyl)thiazol-4-yl)-5-chloro-2-fluorophenyl)propane-1-sulfonamide
InChIKey: VNTBYWJLHBXTEO-UHFFFAOYSA-N
SMILES: CC(C1=NC(C2=C(C(NS(CCC)(=O)=O)=CC(Cl)=C2)F)=C(C3=CC=NC(N)=N3)S1)(C)C
Biological Activity: 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].
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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. | |||||||||||||||||||||
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Keywords