2. MAPK/ERK Pathway Autophagy
  3. Raf Autophagy
  4. Vemurafenib

Vemurafenib  (Synonyms: PLX4032; RG7204; RO5185426)

Cat. No.: HY-12057 Purity: 99.85%
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Vémurafénib (PLX4032) est un inhibiteurde la B-RAF kinase qui est puissant, sélectif et de première classe, avec la IC50s de 31 et 48 nM pour RAFV600E et c-RAF-1, respectivement. Vémurafénib induit une autophagie cellulaire.

Vemurafenib (PLX4032; RG7204; RO5185426) ist ein erstklassiger, selektiver, potenter Inhibitor der B-RAF-Kinase mit IC50s-Werten von 31 bzw. 48 nM für RAFV600E und c-RAF-1. Vemurafenib induziert die autophagy.

Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.

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

Vemurafenib Chemical Structure

Vemurafenib Chemical Structure

CAS No. : 918504-65-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 38 In-stock
10 mg USD 60 In-stock
50 mg USD 140 In-stock
100 mg USD 220 In-stock
500 mg USD 450 In-stock
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Based on 82 publication(s) in Google Scholar

Other Forms of Vemurafenib:

Vemurafenib Related Antibodies

Top Publications Citing Use of Products

74 Publications Citing Use of MCE Vemurafenib

WB

    Vemurafenib purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Jan;39:194-206.  [Abstract]

    Western analysis of related proteins expression with or without the treatment of vemurafenib and other treatments. Left: M6 are transfected with PLAUR siRNA and negative control siRNA and incubated for 48 h in presence of 1 μM vemurafenib. Right: A375 are transfected either with Mock or uPAR overexpressing plasmid pQ2-uPAR. After 24 h are seeded at the same density (800 cells/ml) and cultured in the presence of vemurafenib at indicated concentrations for 10 days.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390.  [Abstract]

    Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with Vemurafenib (1 μM), GSK2118436A (100 nM), or GSK1120212 (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 Oct;37(43):5719-5734.  [Abstract]

    BRAF mutants with in-frame β3-αC loop deletions exhibit a robust but differential inhibitor resistance. Stable fibroblast cells that express individual BRAF mutants with in-frame β3-αC loop deletions are treated with Vemurafenib for 4 h, and p-ERK1/2 is probed by immunoblot and quantified.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Nutrients. 2018 Dec 8;10(12). pii: E1950.  [Abstract]

    Western analysis of protein expression in cells treatmented with or without PLX4032 or RAD001.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Mol Syst Biol. 2017 Jan; 13(1): 905.  [Abstract]

    Western blotting for NGFR-inducible COLO858 cells, NGFRHigh A375 and WM115 cells, and NGFRLow MACSF and MZ7MEL cells, treated for 48 h with 0.2 or 1 μM Vmurafenib or DMSO.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Nov 1;408:43-54.  [Abstract]

    Western blot analysis of p-ERK, ERK, p-AKT and ERK after 24 h of treatment with Vemurafenib. Levels of p-ERK and p-AKT are quantified by densitometric analysis and a corresponding histogram is constructed as relative to ERK or AKT and α-tubulin. Representative Western blot panels on the left.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2017 Jan;95(1):97-108.  [Abstract]

    Immunoblotting of phosphorylated and total EGFR,AKT, and ERK1/2 in A375-M6 clones treated or not with 0.5 μMvemurafenib for 24 h. 50 μL/ well loaded. Tubulin detected as loading control. Quantification (right) of phosphorylated protein on total protein, normalized on housekeeper (Tubulin).

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2013 Feb 1;19(3):598-609.  [Abstract]

    MEKi decreases PD-L1 expression in BRAFi-resistant cells. A, immunoblot analyses of the activities of ERK1/2 and c-Jun in the K028, M34, and K029 parental lines treated with U0126 (U; 20 μM), PLX4032 (PLX; 10 μM), or the combination of U0126 (20 μM) and PLX4032 (10 μM) for 30 minutes. Cells are treated with DMSO (D) as controls. B, immunoblot example showing decrease in PD-L1 expression in parental M34 cells treated with U0126, PLX4032, or the combination.

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    BRaf c-Raf Raf

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

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    Description

    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].

    IC50 & Target[1]

    B-RafV600E

    31 nM (IC50)

    c-Raf-1

    48 nM (IC50)

    In Vitro

    Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells[1]. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells[2]. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032[3].

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

    Vemurafenib Related Antibodies
    In Vivo

    Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts[1]. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts[2].

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

    489.92

    Formula

    C23H18ClF2N3O3S
    CAS No.
    Appearance

    Solid

    Color

    White to gray

    SMILES

    FC1=CC=C(C(F)=C1C(C2=CNC3=NC=C(C=C32)C4=CC=C(C=C4)Cl)=O)NS(CCC)(=O)=O
    Shipping

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

    DMSO : 50 mg/mL (102.06 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 2.0411 mL 10.2057 mL 20.4115 mL
    5 mM 0.4082 mL 2.0411 mL 4.0823 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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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.25 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.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.25 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 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:  1.5% CMC-Na/saline water

      Solubility: 3.33 mg/mL (6.80 mM); Suspended solution; Need ultrasonic

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

    Dosage

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    Number of animals

    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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    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: 99.85%

    COA (249 KB) HNMR (280 KB) RP-HPLC (198 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Briefly, cells are plated in 96-well microtiter plates at a density of 1,000 to 5,000 cells per well in a volume of 180 μL. For the assay, Vemurafenib (RG7204) is prepared at 10 times the final assay concentration in media containing 1% DMSO. Twenty-four hours after cell plating, 20 μL of the appropriate dilution are added to plates in duplicate. The plates are assayed for proliferation 6 days after the cells are plated according to the procedure.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Athymic nude mice, are with ages 13 to 14 weeks, and weighing approximately 23 to 25 g. For the LOX xenografts, 2×106 cells in 0.2 mL of PBS are injected s.c. into the right lateral flank. Vemurafenib (RG7204), formulated as MBP, is suspended at the desired concentration as needed for each dose group in an aqueous vehicle containing 2% Klucel LF and adjusted to pH 4 with dilute HCl. NSC 362856 is of 250-mg capsules. Capsules are opened and combined into one bulk supply. To prepare the stock dosing material, NSC 362856 is first dissolved in 100% DMSO followed by dilution with saline to form a final milky white suspension in 10% DMSO/90% saline (pH 3.4).

    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, 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 2.0411 mL 10.2057 mL 20.4115 mL 51.0287 mL
    5 mM 0.4082 mL 2.0411 mL 4.0823 mL 10.2057 mL
    10 mM 0.2041 mL 1.0206 mL 2.0411 mL 5.1029 mL
    15 mM 0.1361 mL 0.6804 mL 1.3608 mL 3.4019 mL
    20 mM 0.1021 mL 0.5103 mL 1.0206 mL 2.5514 mL
    25 mM 0.0816 mL 0.4082 mL 0.8165 mL 2.0411 mL
    30 mM 0.0680 mL 0.3402 mL 0.6804 mL 1.7010 mL
    40 mM 0.0510 mL 0.2551 mL 0.5103 mL 1.2757 mL
    50 mM 0.0408 mL 0.2041 mL 0.4082 mL 1.0206 mL
    60 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8505 mL
    80 mM 0.0255 mL 0.1276 mL 0.2551 mL 0.6379 mL
    100 mM 0.0204 mL 0.1021 mL 0.2041 mL 0.5103 mL
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    Vemurafenib 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:

    Vemurafenib918504-65-1PLX4032 RG7204 RO5185426PLX 4032PLX-4032RG7204RG 7204RG-7204RO5185426RO 5185426RO-5185426RafAutophagyRaf kinasesInhibitorinhibitorinhibit

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