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

Plixorafenib  (Synonyms: PLX8394; FORE8394)

Cat. No.: HY-18972 Purity: 99.94%
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PLX8394 is a potent and selective BRaf inhibitor, with an IC50 of appr 5 nM for BRAFV600E.

For research use only. We do not sell to patients.

Plixorafenib Chemical Structure

Plixorafenib Chemical Structure

CAS No. : 1393466-87-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 78 In-stock
Solution
10 mM * 1 mL in DMSO USD 78 In-stock
Solid
5 mg USD 65 In-stock
10 mg USD 117 In-stock
25 mg USD 195 In-stock
50 mg USD 325 In-stock
100 mg USD 585 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Plixorafenib Related Antibodies

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).

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    BRaf c-Raf Raf

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1]

    BRafV600E

    5 nM (IC50)

    In Vitro

    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 Related Antibodies
    In Vivo

    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.
    Molecular Weight

    542.53

    Formula

    C25H21F3N6O3S
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (230.40 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 1.8432 mL 9.2161 mL 18.4322 mL
    5 mM 0.3686 mL 1.8432 mL 3.6864 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation

    Purity: 99.94%

    COA (251 KB) HNMR (194 KB) LCMS (647 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [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).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [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.

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

    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

    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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