An orally-available

PLX4720 – 10 mg

Brand:
Cayman
CAS:
918505-84-7
Storage:
-20
UN-No:
Non-Hazardous - /

The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM).{24814} It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases.{24814} PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.{24813,24814,24812}  

 

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Description

An orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM); less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases; induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf

Formal name: N-[3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide

Synonyms:  Raf Kinase Inhibitor V

Molecular weight: 413.8

CAS: 918505-84-7

Purity: ≥95%

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 Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling

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