Vemurafenib (PLX4032, RG7204)

Catalog No.S1267

Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay.

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Vemurafenib (PLX4032, RG7204) Chemical Structure

Vemurafenib (PLX4032, RG7204) Chemical Structure
Molecular Weight: 489.92

Validation & Quality Control

Cited by 67 publications:

14 customer reviews :

Quality Control & MSDS

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Vemurafenib (PLX4032, RG7204) is available in the following compound libraries:

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Product Information

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  • Vemurafenib (PLX4032, RG7204) Mechanism
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay.
Targets SRMS [1]
(Cell-free assay)
ACK1 [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
C-Raf [1]
(Cell-free assay)

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IC50 18 nM 19 nM 31 nM 48 nM
In vitro PLX4032 inhibits B-RAFV600E, C-RAF, as well as wildtype B-RAF, with IC50 of 31 nM, 48 nM and 100 nM, respectively. PLX4032 also inhibits several non-RAF kinases, including ACK1, KHS1, and SRMS, with IC50 of 18 nM to 51 nM. [1] In melanoma cell lines, the inhibitory effect by PLX4032 depends on B-RAF mutational status, because PLX4032 potently inhibits those harboring B-RAF V600 mutants, including V600E, V600D, V600K, and V600R, but not wildtype or other mutants. The IC50 values of PLX4032 on these cells, including MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058, ranges from 20 nM to 1 μM. In these cells, PLX4032 (0.1 μM to 30 μM) also inhibits the phosphorylation of both MEK1/2 and ERK1/2. [2] PLX4032 is highly effective in the treatment of melanoma, for its ability of inhibiting B-RAFV600E. However, PLX4032 displays limited effect in colon cancer patients that also carrying B-RAFV600E oncoprotein. The reason for this is that, in colon cancer cells, B-RAFV600E inhibition by PLX4032 results in a rapid feedback EGFR activation, which compensates for the PLX4032-inhibited cell proliferation. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
8505C (BRAF V600E/V600E)NYewV4t6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWS5OkBpNGLBcoJKSzVyPUW3JI5OKA>?MmjRNlAyPDlzM{[=
SW1736 (BRAF WT/V600E)M2\EWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3HZT|k3KGh?NXTHVpFsUUN3ME2yPUBvVQ>?NX\4TJJJOjBzNEmxN|Y>
BHT101 (BRAF WT/V600E)MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NYLPeFU2QTZiaB?=NETM[HpKSzVyPUm3JI5OMnfaNlAyPDlzM{[=
C643 (HRAS G13R)≥ 500M{LWT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mkf6PVYhcA>?MWfJR|UxKOLLpTC1NFAhdk1?MV:yNFE1QTF|Nh?=
CAL62 (KRAS G12R) > 1000 > 1000NHjRTFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnPMPVYhcA>?NHLnXYZKSzVyPjCxNFAxKG6PMVyyNFE1QTF|Nh?=
TPC-1 (RET/PTC1)M1XXRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MoPwPVYhcA>?M3\JN2lEPTEkibWxNFAxKG6PMV2yNFE1QTF|Nh?=
UKF-NB-3 (ABCB1)NXHhbI54TnWwY4Tpc44hSXO|YYm=M{HTOFEvOjViwsXNNX[y[HJ1OiCqMVPEUXNQNGPOWnlGdmijbnPld{Bi[2O3bYXsZZRqd25ib3[geIhmKG[udX;y[ZNk\W62IFHCR2IyKHO3YoP0doF1\SC{aH;kZY1qdmViMUKzMYOyOFc{PTd4Nh?=
A375 (BRAFV600E)NV3MbolbTnWwY4Tpc44hSXO|YYm=MmixPEBpMlj1SG1UVw>?MmHtTY5kemWjc3XzJIlvfHKjY3XscJVt[XJiUl;TJIFv\CCQTzDs[ZZmdHNiMl;GNlU{PjN4NES=

... Click to View More Cell Line Experimental Data

In vivo In B-RAFV600E-mutant mice xenograft models, PLX4032 (6 mg/kg–20 mg/kg) inhibits tumor growth. [1] In mice xenograft models of LOX, Colo829, and A375 cells, PLX4032 (12.5 mg/kg–100 mg/kg) inhibits tumor growth and prolongs mice survival. [2]
Features A novel and potent inhibitor of the B-RAFV600E oncoprotein.

Protocol(Only for Reference)

Kinase Assay: [1]

RAF kinase activity measurements The kinase activities of wild-type RAF and mutants are determined by measuring phosphorylation of biotinylated-BAD protein. For each enzyme (0.01 ng), 20 μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% (v/v) Tween-20, 50 nM biotin-BAD protein, and 1 mM ATP at room temperature. Reactions are stopped at 5 min with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 0.3% (w/v) bovine serum albumin (BSA). The stop solution also includes phospho-BAD (Ser112) antibody, streptavidin-coated donor beads, and protein A acceptor beads. The antibody and beads are pre-incubated in stop solution in the dark at room temperature for 30 min. The final dilution of antibody is 1/2000 and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour and then are read on a PerkinElmer AlphaQuest reader. Mutant activities are the average of two different batches of purified protein assayed in duplicate in three different experiments.

Cell Assay: [2]

Cell lines MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058 cells
Concentrations 0–10 μM , dissolved in DMSO
Incubation Time 5 days
Method Cellular proliferation is evaluated by MTT assay. Briefly, cells are plated in 96-well microtiter plates at a density of 1000 to 5000 cells per well in a volume of 180 μL. PLX4032 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 of PLX4032 are added to plates in duplicate. The plates are assayed for proliferation 6 days after the cells are plated. Percent inhibition is calculated and the IC50 is determined from the regression of a plot of the logarithm of the concentration versus percent inhibition.

Animal Study: [2]

Animal Models Mice (athymic nude) xenograft models of LOX, Colo829, and A375 cells
Formulation Formulated as microprecipitated bulk powder (MBP), suspended at the desired concentration in an aqueous vehicle containing 2% Klucel LF, and adjusted to pH 4 with dilute HCl
Dosages 12.5 mg/kg–100 mg/kg
Administration Oral gavage twice daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Bollag G, et al. Nature, 2010, 467(7315), 596-599.

[2] Yang H, et al. Cancer Res, 2010, 70(13), 5518-5527.

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Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02314481 Not yet recruiting Non-small Cell Lung Cancer University College, London|Hoffmann-La Roche January 2017 Phase 2
NCT02721459 Not yet recruiting Melanoma|Skin Cancer H. Lee Moffitt Cancer Center and Research Institute|Exeli  ...more H. Lee Moffitt Cancer Center and Research Institute|Exelixis|Genentech, Inc. September 2016 Phase 1
NCT01843738 Not yet recruiting BRAFV600 Mutation|Stage IV Melanoma University of Utah August 2016 Phase 1
NCT02818023 Recruiting Melanoma University of Pittsburgh|Merck Sharp & Dohme Corp. July 2016 Phase 1
NCT02768207 Recruiting Metastatic Melanoma, BRAF V600 Mutation Positive Hoffmann-La Roche May 2016 Phase 2

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Chemical Information

Download Vemurafenib (PLX4032, RG7204) SDF
Molecular Weight (MW) 489.92


CAS No. 918504-65-1
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms RO5185426
Solubility (25°C) * In vitro DMSO 97 mg/mL (197.99 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-​[3-​[[5-​(4-​chlorophenyl)​-​1H-​pyrrolo[2,​3-​b]​pyridin-​3-​yl]​carbonyl]​-​2,​4-​difluorophenyl]​-1-​propanesulfonamide

Frequently Asked Questions

  • Question 1
    How about the half-life of Vemurafenib(S1267)?

    Answer: It was reported that the half-life of the compound is 57 hours.

  • Question 2
    The vemurafenib power, when prepared in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O solutions, form a pellet down the tube?

    Answer: When prepare this kind of vehicle, please dissolve the drug in DMSO clearly first. If it dissolves not readily, please sonicate and warm in the water bath at about 45 degree. Then add PEG and Tween. After they mixed homogeneously, then dilute with water.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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