GDC 0879

• Supplier: Tocris Bioscience
• Catalog: 4554
• Prices: $225.00, $925.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 905281-76-7
• Chemical Name: (E)-2,3-Dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-oneoxime
• Formula: C19H18N4O2
• Molecular Weight: 334.37
• Purity: >98 %
• Description: Potent and selective B-Raf inhibitor (IC 50 = 0.13 nM against purified B-Raf V600E ). Activity reduces phospho-ERK (pERK) levels (IC 50 = 63 nM in the Malme-3M cell line). Inhibits the Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines. Does not activate apoptotic pathways in A375 or Colo205 cell lines. Orally bioavailable.

Product References

Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E - Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E

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. Cancer Res. 2009 Apr 1;69(7):3042-51.

Pharmacodynamics of - Pharmacodynamics of

Wong H, Belvin M, Herter S, Hoeflich KP, Murray LJ, Wong L, Choo EF. J Pharmacol Exp Ther. 2009 Apr;329(1):360-7.

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance - RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance

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. Nature. 2010 Mar 18;464(7287):431-5.