2. MAPK/ERK Pathway
  3. Raf
  4. Plixorafenib

Plixorafenib  (Synonyms: PLX8394; FORE8394)

製品番号: HY-18972 純度: 99.10%
COA 取扱説明書 Technical Support

PLX8394 is a potent and selective BRaf inhibitor, with an IC50 of appr 5 nM for BRAFV600E.

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CAS 番号 : 1393466-87-9

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 78 在庫あり
Solution
10 mM * 1 mL in DMSO USD 78 在庫あり
Solid
5 mg $65 在庫あり
10 mg $117 在庫あり
25 mg $195 在庫あり
50 mg $325 在庫あり
100 mg $585 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 20 publication(s) in Google Scholar

Plixorafenib 関連抗体

Top Publications Citing Use of Products

    Plixorafenib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Sep;8(9):1130-1141.  [Abstract]

    BRAF V600E or V600E/L514V are transiently transfected in SKBR3 for 24 hr. Then the cells are treated with 1 μM GW572016 for 1 hr, followed by treatment with DMSO or the RAF inhibitors indicated for 1 hr (the dose for PLX7904 is 1 μM).

    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
    B-Raf 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

    PLX8394 is a potent and selective BRaf inhibitor, with an IC50 of appr 5 nM for BRAFV600E.

    IC50 & Target[1]

    BRafV600E

    5 nM (IC50)

    体外実験

    PLX8394 potently inhibits phosphorylation of ERK1/2 in PRT #3 and PRT #4 cells at >25 nM and in addition to parental cells at 10 nM. PLX8394 effectively reduces cyclin D3 and cyclin D1, phosphorylation of retinoblastoma protein, and expression of cyclin A2 in parental cells and PRT #3 and PRT #4 cells. PLX8394 inhibits ERK1/2 phosphorylation and the growth of PLX4032-resistant cells harboring either a BRAF V600K/L505H double mutation or an transposon-induced, N-terminal truncated form of BRAF[1]. PLX8394 significantly impairs tumor cell growth and suppresses MAPK signaling in LA cell lines expressing either endogenous V600E or non-V600 mutant forms of BRAF[2].

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

    Plixorafenib 関連抗体
    体内実験

    PLX8394 (150 mg/kg/d) substantially suppresses tumor growth, MAPK pathway signaling and tumor cell proliferation in these H1755 xenograft tumors without overt toxicity in mice. PLX8394 combines with CP-358774 yields plasma CP-358774 concentrations of >1 μM[2].

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

    542.53

    分子式

    C25H21F3N6O3S
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(C1=C(F)C(NS(=O)(N2CC[C@@H](F)C2)=O)=CC=C1F)C3=CNC4=C3C=C(C=N4)C5=CN=C(C6CC6)N=C5
    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 : 100 mg/mL (184.32 mM; ultrasonic and warming and heat to 60°C; 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 1.8432 mL 9.2161 mL 18.4322 mL
    5 mM 0.3686 mL 1.8432 mL 3.6864 mL
    10 mM 0.1843 mL 0.9216 mL 1.8432 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

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    体積 （開始）

    V1

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    濃度 （終了）

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    V2

    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    90% Corn Oil

      Solubility: ≥ 5 mg/mL (9.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    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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    % 
    +
    %
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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: 99.80%

    COA (251 KB) HNMR (217 KB) LCMS (467 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    For MTT assays, 2×103 cells are seeded in triplicate in 96 wells in their regular culture medium (containing PLX4720 for PRT lines). Next day, cells are washed twice with PBS and then the medium is replenished containing the indicated RAF inhibitor. Medium is changed 48 hours later and after a further 48 hours, 10 μL of 5 mg/mL MTT reagent is added to wells, and incubated for three hours. Formazan crystals are then solubilized overnight with a 1:10 dilution of 0.1 M glycine (pH 10.5) in DMSO. Wells are then analyzed at 450 nM in a Multiskan® Spectrum spectrophotometer. Results depicted are normalized to DMSO conditions and are a composite of three independent experiments. Error bars shown are representative of the standard error of mean (SEM).

    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]

    H1755 tumor xenografts are generated by injection of 5×106 cells in a 50/50 mixture for matrigel and PBS into 6- to 8-wk-old female NOD/SCID mice. Mice are randomized to treatment groups once tumors reach an average size of 150 mm3. H1755 cells are s.c. implanted and allowed to grow to appr 200 mm3 (4 wk after implantation). Mice are then treated with vehicle, PLX4032, or PLX8394 for 15 d. The vehicle for daily oral gavage is PEG 400 [20% (vol/vol)], tocopheryl polyethylene glycol succinate (TPGS) [5% (vol/vol)], water [75% (vol/vol)]. PLX8394 is dissolved in PEG 400 [20% (vol/vol)], TPGS [5% (vol/vol)], and water [75% (vol/vol)] and vortexed continuously throughout the dosing period. PLX8394 is given daily by oral gavage at a dose of 150 mg/kg/d.

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8432 mL 9.2161 mL 18.4322 mL 46.0804 mL
    5 mM 0.3686 mL 1.8432 mL 3.6864 mL 9.2161 mL
    10 mM 0.1843 mL 0.9216 mL 1.8432 mL 4.6080 mL
    15 mM 0.1229 mL 0.6144 mL 1.2288 mL 3.0720 mL
    20 mM 0.0922 mL 0.4608 mL 0.9216 mL 2.3040 mL
    25 mM 0.0737 mL 0.3686 mL 0.7373 mL 1.8432 mL
    30 mM 0.0614 mL 0.3072 mL 0.6144 mL 1.5360 mL
    40 mM 0.0461 mL 0.2304 mL 0.4608 mL 1.1520 mL
    50 mM 0.0369 mL 0.1843 mL 0.3686 mL 0.9216 mL
    60 mM 0.0307 mL 0.1536 mL 0.3072 mL 0.7680 mL
    80 mM 0.0230 mL 0.1152 mL 0.2304 mL 0.5760 mL
    100 mM 0.0184 mL 0.0922 mL 0.1843 mL 0.4608 mL
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    Plixorafenib Related Classifications

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    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:

    Plixorafenib1393466-87-9PLX8394 FORE8394PLX 8394PLX-8394FORE8394FORE 8394FORE-8394RafRaf kinasesInhibitorinhibitorinhibit

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