A selective inhibitor of B-RafV600E mutant melanoma cell proliferation (EC50 = 4 nM) with little activity against wild-type B-Raf or a panel of 100 other kinases (IC50s = 900 nM); decreases phosphorylation of the B-Raf substrate MEK at oral doses of 6 mg/kg in human melanoma xenograft models

Encorafenib – 5 mg

Brand:
Cayman
CAS:
1269440-17-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling. A mutation of B-Raf in exon 15 at codon 600 where a valine is substituted by glutamic acid (V600E) has been linked to melanoma.{27148} Encorafenib is a selective inhibitor of B-RafV600E mutant melanoma cell proliferation (EC50 = 4 nM) with little activity against wild-type B-Raf or a panel of 100 other kinases (IC50s = 900 nM).{27851} At oral doses of 6 mg/kg in human melanoma xenograft models, encorafenib was shown to decrease phosphorylation of the B-Raf substrate MEK.{27852}  

 

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Description

A selective inhibitor of B-RafV600E mutant melanoma cell proliferation (EC50 = 4 nM) with little activity against wild-type B-Raf or a panel of 100 other kinases (IC50s = 900 nM); decreases phosphorylation of the B-Raf substrate MEK at oral doses of 6 mg/kg in human melanoma xenograft models

Formal name: N-[(1S)-2-[[4-[3-[5-chloro-2-fluoro-3-[(methylsulfonyl)amino]phenyl]-1-(1-methylethyl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]-1-carbamic acid, methyl ester

Synonyms:  LGX818

Molecular weight: 540

CAS: 1269440-17-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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