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

Vemurafenib (Synonyms: PLX4032; RG7204; RO5185426)

Cat. No.: HY-12057 Purity: 99.80%
Handling Instructions

Vemurafenib (PLX4032; RG7204) 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.

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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 108 In-stock
Estimated Time of Arrival: December 31
100 mg USD 144 In-stock
Estimated Time of Arrival: December 31
200 mg USD 252 In-stock
Estimated Time of Arrival: December 31
500 mg USD 420 In-stock
Estimated Time of Arrival: December 31
1 g USD 696 In-stock
Estimated Time of Arrival: December 31
5 g   Get quote  
10 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 31 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Vemurafenib purchased from MCE. Usage Cited in: Cancer Lett. 2017 Nov 1;408:43-54.

    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 MCE. Usage Cited in: Clin Cancer Res. 2013 Feb 1;19(3):598-609.

    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.

    Vemurafenib purchased from MCE. Usage Cited in: Mol Syst Biol. 2017 Jan; 13(1): 905.

    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 MCE. Usage Cited in: J Mol Med (Berl). 2017 Jan;95(1):97-108.

    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 MCE. Usage Cited in: Oncogene. 2018 Oct;37(43):5719-5734.

    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 MCE. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390.

    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 MCE. Usage Cited in: Nutrients. 2018 Dec 8;10(12). pii: E1950.

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

    Vemurafenib purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jan;39:194-206.

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Vemurafenib (PLX4032; RG7204) 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.

    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].

    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].

    Clinical Trial
    Molecular Weight

    489.92

    Formula

    C₂₃H₁₈ClF₂N₃O₃S

    CAS No.

    918504-65-1

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 6.2 mg/mL (12.66 mM; Need ultrasonic and warming)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.2041 mL 1.0206 mL 2.0411 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.10 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.80%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    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

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Vemurafenib
    Cat. No.:
    HY-12057
    Quantity: