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

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
1 mg USD 42 在庫あり
5 mg USD 90 在庫あり
10 mg USD 140 在庫あり
25 mg USD 280 在庫あり
50 mg USD 450 在庫あり
100 mg USD 720 在庫あり
200 mg   お問い合わせ  
500 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

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

GDC-0879 関連抗体

Top Publications Citing Use of Products

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

    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.

    Raf アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    BRaf c-Raf Raf

    • 生物活性

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    • 純度とドキュメンテーション

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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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    GDC-0879 関連抗体
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    334.37

    分子式

    C19H18N4O2
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to light brown

    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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na  0.5% Tween-80

      Solubility: 3.23 mg/mL (9.66 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.69%

    COA (250 KB) LCMS (267 KB)

    取扱説明書 (2659 KB)
    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].

    MedChemExpress (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].

    MedChemExpress (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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.9907 mL 14.9535 mL 29.9070 mL 74.7675 mL
    5 mM 0.5981 mL 2.9907 mL 5.9814 mL 14.9535 mL
    10 mM 0.2991 mL 1.4953 mL 2.9907 mL 7.4767 mL
    15 mM 0.1994 mL 0.9969 mL 1.9938 mL 4.9845 mL
    20 mM 0.1495 mL 0.7477 mL 1.4953 mL 3.7384 mL
    25 mM 0.1196 mL 0.5981 mL 1.1963 mL 2.9907 mL
    30 mM 0.0997 mL 0.4984 mL 0.9969 mL 2.4922 mL
    40 mM 0.0748 mL 0.3738 mL 0.7477 mL 1.8692 mL
    50 mM 0.0598 mL 0.2991 mL 0.5981 mL 1.4953 mL
    60 mM 0.0498 mL 0.2492 mL 0.4984 mL 1.2461 mL
    80 mM 0.0374 mL 0.1869 mL 0.3738 mL 0.9346 mL
    100 mM 0.0299 mL 0.1495 mL 0.2991 mL 0.7477 mL
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    GDC-0879 Related Classifications

    • Molarity Calculator

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GDC-0879905281-76-7GDC0879GDC 0879RafRaf kinasesInhibitorinhibitorinhibit

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