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    GDC-0879
    GDC-0879

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1005
    CAS #: 905281-76-7Purity ≥98%

    Description: GDC-0879 (AR-00341677; GDC-0879; AR00341677) is a novel, potent, highly selective, and orally bioavailable B-Raf kinase inhibitor with potential antitumor activity. It inhibits B-Raf kinase with an IC50 of 0.13 nM in A375 and Colo205 cells. In mice treated with GDC-0879, both cell line- and patient-derived BRAF(V600E) tumors exhibited stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared with mutant KRAS-expressing tumors. The Raf/mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase signaling pathway is involved in cellular responses relevant to tumorigenesis, including cell proliferation, invasion, survival, and angiogenesis. 

    References: Arch Pharm Res. 2011 May;34(5):699-701;  2009 Apr;329(1):360-7.

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    Molecular Weight (MW)334.37
    FormulaC19H18N4O2
    CAS No.905281-76-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 66 mg/mL warming (197.4 mM)
    Water: <1 mg/mL
    Ethanol: 5 mg/mL (14.95 mM)
    Solubility (In vivo)0.5% methylcellulose+0.2% Tween 80: 8 mg/mL
    SynonymsAR 00341677; GDC0879; AR00341677; AR-00341677; GDC-0879; GDC 0879


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    In Vitro

    In vitro activity: GDC-0879 also inhibits cellular pERK with IC50 of 63 nM. GDC-0879 shows comparable potency in A375 melanoma and Colo205 colorectal carcinoma cell lines, both of which are B-RafV600E mutant, with IC50 of 59 nM and 29 nM for pMEK1 inhibition respectively. GDC-0879 potently inhibits B-RafV600E in Malme3M cells with IC50 of 0.75 μM. GDC-0879 also shows EC50 values < 0.5 μM in many tumor cells (A375, 624, SK-MEL-28, Malme3M, C32, 928, 888, G-361, Colo205, Colo206, SW1417, CL34, and Colo201).


    Kinase Assay: GDC-0879 is a potent and selective B-Raf inhibitor with an IC50 of 0.13 nM.


    Cell Assay: GDC-0879 in vitro IC50 estimates for pMEK inhibition are determined using A375 and Colo205 cells. In brief, A375 or Colo205 cells are incubated with a range of GDC-0879 concentrations (from 0.5 nM to 6.75 μM) for 25 min. Cells are lysed, and the lysates are subjected to centrifugation at 16,100g for 30 min, and the level of total protein is determined. Enzyme-linked immunosorbent assay kits are used to determine pMEK1 and total MEK1 protein levels in a 96-well format. Samples are analyzed in duplicate at 20 μg of protein per well. The optical densities obtained at 450 nm are converted to units per milliliter (for pMEK1) or nanograms per milliliter (for total MEK1) using a standard curve determined with recombinant pMEK1 or MEK1. The pMEK1/total MEK1 ratios are then calculated as units per nanogram. The IC50 estimates for pMEK1 inhibition are estimated by nonlinear regression using GraphPad Prism version 4.02.

    In VivoIn GDC-0879 treated mice, both cell line- and patient-derived BRAFV600E tumors exhibit stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared to mutant KRAS-expressing tumors. Although there is involvement of activated RAF signaling in RAS-induced tumorigenesis, decreased time to progression is observed for some KRAS-mutant tumors following GDC-0879 administration. Whereas GDC-0879-mediated efficacy is associated strictly with B-RafV600E status, MEK inhibition also attenuates proliferation and tumor growth of cell lines expressing wild-type BRAF (81% KRAS mutant, 38% KRAS wild type). The responsiveness of B-RafV600E melanoma cells to GDC-0879 could be dramatically altered by pharmacologic and genetic modulation of PI3K pathway activity.
    Animal modelFemale nu/nu mice
    Formulation & DosageFormulated in 0.5% methylcellulose/0.2% Tween 80; 100 mg/kg; p.o.
    References[1] Wong H, et al. J Pharmacol Exp Ther. 2009, 329(1), 360-367.[2] Hoeflich KP, et al. Cancer Res. 2009, 69(7), 3042-3051.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    GDC-0879

    GDC-0879 is a potent and selective RAF kinase inhibitor. Cancer Res. 2009 Apr 1;69(7):3042-51.

    GDC-0879

    BRAFV600E mutation predicts for enhanced sensitivity of melanoma, colon, and lung cancer cell lines to RAF inhibitors in vitro.

    GDC-0879

    Wild-type BRAF melanoma tumors have an attenuated pharmacodynamic response to GDC-0879 treatment relative to BRAFV600E tumor xenografts.


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