An inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme); selective for B-RafV600E over a panel of 140 kinases at 1 μM; inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that express B-RafV600E (IC50s = 29 and 59 nM

GDC 0879 – 10 mg

Brand:
Cayman
CAS:
905281-76-7
Storage:
-20
UN-No:
Non-Hazardous - /

GDC 0879 is an inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme).{27943} It is selective for B-RafV600E over a panel of 140 kinases at a concentration of 1 μM. GDC 0879 inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that express B-RafV600E (IC50s = 29 and 59 nM, respectively). In vivo, GDC 0879 (15-200 mg/kg) inhibits tumor growth in a dose-dependent manner in an A375 mouse xenograft model.  

 

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Description

An inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme); selective for B-RafV600E over a panel of 140 kinases at 1 μM; inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that express B-RafV600E (IC50s = 29 and 59 nM, respectively); inhibits tumor growth in an A375 mouse xenograft model from 15-200 mg/kg

Formal name: 2,3-dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one, oxime

Synonyms: 

Molecular weight: 334.4

CAS: 905281-76-7

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 Signaling|ERK/MAPK Signaling

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