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Vemurafenib (PLX4032)

Cat. No. M1761
Vemurafenib (PLX4032) Structure

RG7204; RO5185426

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 30  USD30 In stock
10mg USD 37  USD37 In stock
25mg USD 70  USD70 In stock
50mg USD 100  USD100 In stock
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Quality Control & Documentation
Biological Activity

Vemurafenib (PLX4032) is the first and effective selective inhibitor of B-Raf, which can inhibit RAFV600E and C-RAF-1 activity with IC50 of 31 nM and 48 nM, respectively. Vemurafenib induces autophagy.

Product Citations
Customer Product Validations & Biological Datas
Source Cell Death Differ (2016). Figure 2. PLX4032
Method western blot
Cell Lines BRAF mutant melanoma cell lines
Concentrations 3 μM
Incubation Time 24 h
Results PLX4032-induced upregulation of BIM and PUMA occurred normally in the control sgRNA transduced cell lines.
Source Cell Death Differ (2016). Figure 1. PLX4032
Method flow cytometry
Cell Lines BRAFWT cells
Concentrations 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time 24 h
Results We found that PLX4032 induced significant dose-dependent apoptosis over a time course of 5 days in all BRAF mutant melanoma cell lines (M14, UACC257, Malme3M, SKMEL5 and UACC62), whereas the BRAFWT cells (CHL-1) were unaffected.
Protocol (for reference only)
Cell Experiment
Cell lines MDA-MB-435 cells line
Preparation method Cellular proliferation assays Cellular proliferation was evaluated by 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT; Sigma) assay. Briefly, cells were 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, RG7204 was 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 were added to plates in duplicate. The plates were assayed for proliferation 6 days after the cells were plated according to the procedure originally described by Mosmann . The IC50 was determined from the regression of a plot of the logarithm of the concentration versus percent inhibition by XLfit (version 4.2; IDBS) using the Dose-Response One-Site Model (#205).
Concentrations 0~10µM
Incubation time 6 days
Animal Experiment
Animal models Colo829 and A375 xenografts
Formulation an aqueous vehicle containing 2% Klucel LF (Hydroxypropylcellulose; Aqualon) and adjusted to pH 4 with dilute HCl.
Dosages 100 mg/kg bid
Administration oral gavage
Chemical Information
Molecular Weight 489.92
Formula C23H18ClF2N3O3S
CAS Number 918504-65-1
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Shao Y et al. Cell Death Differ. BH3-only protein silencing contributes to acquired resistance to PLX4720 in human melanoma.

[2] Patrawala S et al. Future Oncol. Vemurafenib (RG67204, PLX4032): a potent, selective BRAF kinase inhibitor.

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Vemurafenib (PLX4032; RG7204; RO5185426) is a first-in-class selective B-RAF inhibitor that inhibits the activity of RAFV600E and c-RAF-1 with IC50 at 31 nM and 48 nM, respectively.


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Abmole Inhibitor Catalog

Keywords: Vemurafenib (PLX4032), RG7204; RO5185426 supplier, Raf, inhibitors, activators

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