kinases protein kinase inhibitors signaling activators kinase substrates antibodies bioluminescence assays
B-RAF protein kinase inhibitor GDC 0879, 2 mg  

B-RAF protein kinase inhibitor GDC 0879, 2 mg

B-Raf inhibitor, (E)-5-[1-(2-Hydroxy-ethyl)-3-pyridin-4-yl-1H-pyrazol-4-yl]-indan-1-one oxime

potent inhibitor of B-Raf, protein inhibitor, GDC-0879

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Availability: within 3 days

110,50 €

Background: GDC-0879 is a novel, potent, selective and orally bioavailable B-Raf inhibitor with IC50 values in the B-RAF (V600E) (enzyme assay) and MALME-3M pERK assay (tumour cell-based assay) of 0.13 and 63 nM, respectively. Furthermore, the compound has shown in vivo efficacy in various mouse xenograft models carrying the V600E mutation.

Purity: > 99%
Solubility: DMSO to 100 mM
Molecular Weight:  334.5 g/mol
Formula: C19H18N4O2
CAS number: 905281-76-7
Appearance: White solid
Manufacturer: Axon Medchem

Product specific literature references:

Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M, Friedman LS, Malek S. (2010) “RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.” Nature. 18; 464(7287):431-5.

Hoeflich KP, Herter S, Tien J, Wong L, Berry L, Chan J, O\'Brien C, Modrusan Z, Seshagiri S, Lackner M, Stern H, Choo E, Murray L, Friedman LS, Belvin M.(2009) “Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression.” Cancer Res. 69(7):3042-51.

Choo EF, Driscoll JP, Feng J, Liederer B, Plise E, Randolph N, Shin Y, Wong S, Ran Y. (2009) “Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species.” Xenobiotica. 39(9):700-9.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.