1. MAPK/ERK Pathway
  2. Raf
  3. GDC-0879

GDC-0879 

製品番号: HY-50864 純度: 99.94%
取扱説明書

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

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GDC-0879 構造式

GDC-0879 構造式

CAS 番号 : 905281-76-7

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 132 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 72 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 216 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 396 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 708 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GDC-0879 purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.
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    製品説明

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

    IC50 & Target[1]

    B-Raf

    0.13 nM (IC50)

    体外実験

    GDC-0879 also inhibits pERK with an IC50 of 63 nM[1]. GDC-0879 represents a novel potent and selective B-Raf inhibitor that is being evaluated as a potential antitumor agent. GDC-0879 exhibits potent inhibition of Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines with low cellular pMEK1 inhibition IC50 estimates of 59 and 29 nM in A375 melanoma and Colo205 colorectal carcinoma cells, respectively[2].

    体内実験

    The pharmacokinetic parameters of GDC-0879 after oral administration of 15, 25, 50, 100, and 200 mg/kg in MCT in mice are estimated as follows: ka=8.20 h-1, ke=0.59 h-1, and apparent volume of distribution=6.19 L/kg[2].

    分子量

    334.37

    分子式

    C₁₉H₁₈N₄O₂

    CAS 番号

    905281-76-7

    SMILES

    O/N=C1C(C=CC(C2=CN(CCO)N=C2C3=CC=NC=C3)=C4)=C4CC/1

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (149.53 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9907 mL 14.9535 mL 29.9070 mL
    5 mM 0.5981 mL 2.9907 mL 5.9814 mL
    10 mM 0.2991 mL 1.4953 mL 2.9907 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (7.48 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.48 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [2]

    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[2].

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [2]

    Mice[2]
    Female athymic nu/nu mice (weighing 25-28 g) are administered oral doses of 15, 25, 50, 100, and 200 mg/kg GDC-0879. Blood samples (~1 mL) are collected at 0.5, 1, 2, 4, 8, and 24 h after dose via cardiac puncture (terminal collection) into tubes containing K2EDTA anticoagulant. Immediately upon collection, the blood is mixed with K2EDTA and stored on ice. Within 30 min, blood samples are centrifuged at approximately 1000 to 1500g for 5 min at 4°C, and plasma is harvested. The plasma samples are stored at -80°C until analysis[2].

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献
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    Keywords:

    GDC-0879GDC0879GDC 0879RafRaf kinasesInhibitorinhibitorinhibit

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    製品名:
    GDC-0879
    製品番号:
    HY-50864
    数量:
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