Vemurafenib (PLX4032, RG7204)

Catalog No.S1267 Synonyms: RO5185426

Vemurafenib (PLX4032, RG7204) Chemical Structure

Molecular Weight(MW): 489.92

Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold.

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Cited by 83 Publications

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Biological Activity

Description Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold.
Features A novel and potent inhibitor of the B-RAFV600E oncoprotein.
Targets
SRMS [1]
(Cell-free assay)		 ACK1 [1]
(Cell-free assay)		 B-Raf (V600E) [1]
(Cell-free assay)		 C-Raf [1]
(Cell-free assay)		 MAP4K5 (KHS1) [1]
(Cell-free assay)
18 nM 19 nM 31 nM 48 nM 51 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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 MknPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[xNFAh|ryP NVK3ZmxYQTZiaB?= MlzhSG1UVw>? NEjXcWRKSzVyPUS3JI5O MniyNVg1PThyNUO=
ARO NHmwe|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIT5U2syODBizszN Ml3tPVYhcA>? NEnCWldFVVOR MWPJR|UxRTJyNTDuUS=> NWnMRnhMOTh2NUiwOVM>
NPA NGLIXmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rvUlExOCEQvF2= NWLQXoJ2QTZiaB?= NHvGOpNFVVOR Moq3TWM2OD1{NjDuUS=> M2TyZVE5PDV6MEWz
TPCI NV7JPXIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\HVnV4OTByIN88US=> M1noclk3KGh? M3rzWmROW09? M{T6UmlEPTB;MUCuO|ch|ryP Mnn3NVg1PThyNUO=
A375 Mni2RZBweHSxc3nzJGF{e2G7 MnfsNVAh|ryP NWfINWNjTE2VTx?= MV7Qdo9ud3SnczDhdI9xfG:2aXOg[IVifGh? NX33OFRHOTh2NUiwOVM>
ARO M{LrZWZ2dmO2aX;uJGF{e2G7 NVSyWXI4OTBizszN NF3U[W04OiCq NHfPNHBFVVOR NFvRfZpKdmS3Y3XzJJRp\SC{ZXX4dJJme3Orb36gc4YhfGinIF7JV{BxfW2y NFzUNlAyQDR3OEC1Ny=>
8505C (BRAF V600E/V600E) NUDE[FJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVe5OkBp NXLlTnE{UUN3ME21O{BvVSB? NEnzNpEzODF2OUGzOi=>
SW1736 (BRAF WT/V600E) MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVK5OkBp MYfJR|UxRTJ7IH7N NUDYS2lZOjBzNEmxN|Y>
BHT101 (BRAF WT/V600E) NEezcG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYS5OkBp MmTMTWM2OD17NzDuUS=> NFLDWGozODF2OUGzOi=>
BCPAP (BRAF WT/V600E) M4\XVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfpPVYhcA>? NYL6XnR5UUN3ME23PEBvVQ>? M1LqZVIxOTR7MUO2
C643 (HRAS G13R)≥ 500 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zDXFk3KGh? MnHRTWM2OCEkibWgOVAxKG6P M1TselIxOTR7MUO2
HTH7 (NRAS Q61R) MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3x[5M6PiCq MoDTTWM2OOLLpTCxNFAxKG6P NH\QW3IzODF2OUGzOi=>
CAL62 (KRAS G12R) > 1000 > 1000 NX73VW1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn1WpI6PiCq M1fF[2lEPTB-IEGwNFAhdk1? NVvYeFdQOjBzNEmxN|Y>
TPC-1 (RET/PTC1) MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkSzPVYhcA>? NGnkTpRKSzVy4polNVAxOCCwTR?= NE\aUVgzODF2OUGzOi=>
PC MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnWPVYhcA>? M33rPGlEPTB-IEGwNFAhdk1? NVLaSWVtOjBzNEmxN|Y>
Calu-6 NGLSbY9HfW6ldHnvckBCe3OjeR?= Ml\rNgKBkc7:TR?= MnzWNUBp MYDEUXNQ NXmyRo03SWO2aY\heIV{KE2HSz;FVmshcW5iY3XscJMhf2m2aDD3bYxlNXS7cHWgRnJCTg>? MYmyNFE4QTdyNR?=
C4 NFHYb5RHfW6ldHnvckBCe3OjeR?= NV\zNHQyOyEQvF2= NXjleZZxPDhiaB?= NImxWZNFVVOR MX;JcoNz\WG|ZYOgZ49tdGGpZX6gd5lvfGinc3nzJIFv\CCmZXPy[YF{\XNiSVytPEBmgHC{ZYPzbY9v M1O5SVI2QTh7NUC2
VMM12 MYLGeY5kfGmxbjDBd5NigQ>? M{\2RVMh|ryP NYL4U4FUPDhiaB?= MXHEUXNQ NEHROnNKdmO{ZXHz[ZMh[2:ubHHn[Y4he3mwdHjld4l{KGGwZDDk[YNz\WG|ZYOgTWwuQSCneIDy[ZN{cW:w M1e5dFI2QTh7NUC2
SKMEL19 M{jE[WZ2dmO2aX;uJGF{e2G7 MV62JO69VQ>? Mn30OFghcA>? MkHZSG1UVw>? M3T3Z3RzcWepZYLzJGVTKHO2cnXzdy=> M1fXTFI{OzZ{MkSw
UKF-NB-3 (ABCB1) NXHvXm5QTnWwY4Tpc44hSXO|YYm= MVyxMlI2KML3TR?= MXGyJIg> M3HWTmROW09? NWCwN5BtTW6qYX7j[ZMh[WOldX31cIF1cW:wIH;mJJRp\SCobIXvdoV{[2WwdDDBRmNDOSC|dXLzeJJifGVicnjv[IFucW6nIEGyNy=> M37MbVI1PzN3N{[2
UKF-NB-3 NIPGUWhHfW6ldHnvckBCe3OjeR?= Mn;mNU4zPSEEtV2= MnT6NkBp M3[2XmROW09? NWC1e2M4W2mpbnnmbYNidnSueTDh[oZm[3S|IH;uJIFk[3WvdXzheIlwdiCxZjD0bIUh\my3b4Lld4NmdnRiQVLDRlEhe3Wkc4TyZZRmKHKqb3ThcYlv\SBzMkO= NX\KR|FGOjR5M{W3OlY>
A375 (BRAFV600E) NIPES5FHfW6ldHnvckBCe3OjeR?= MV[4JIg> NI\aXmNFVVOR M3vZSmlv[3KnYYPld{BqdnS{YXPlcIx2dGG{IGLPV{BidmRiTl:gcIV3\Wy|IB?= NYLmWHdsOjV|NkO2OFQ>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-ERK / p-CRAF; 

PubMed: 22448344     


BRAF mutant cell lines from (A) were treated with 3µM vemurafenib for the indicated times, and lysates were probed with the indicated antibodies.

p-MEK(S217/221) / pAKT(T308) / p-AKT(S473) / p-P70 S6K(T389) / p-S6(Ser235-236) / P-4EB-P1; 

PubMed: 22194965     


Western blot analysis of phosphorylated and the total amount of key proteins in the MAPK and PI3K/AKT pathways after 24 hours of exposure to the solvent (DMSO), or various concentrations of the BRAF inhibitor vemurafenib. The vemurafenib-sensitive M238 and M229 cell lines and the vemurafenib in vitro acquired resistant sublines M238-AR2 and M229-AR9 were cultured at different concentrations of vemurafenib. p70 and p-p70 S6K in this figure are referred to S6K1 and phosphorylated form of S6K1, respectively.

Bax / Bcl2 / Bcl-xl / BIM / Mcl1; 

PubMed: 28382170     


Change of Bcl-2 family proteins following Vemurafenib treatment for 24 h.

22448344 22194965 28382170
Growth inhibition assay
Cell viability; 

PubMed: 29179510     


At different time point of the experiment (expressed in days), sensitivity to vemurafenib was evaluated in the different A375 cell lines. Cells were treated with 10-fold dilution series (1 nM to 10 uM) of Vemurafenib and cell viability was assessed after 72 h by Crystal violet staining. Cell viability results are expressed in fold vs. the untreated cells.

29179510
Immunofluorescence
uPAR / α5-β1; 

PubMed: 30611716     


Representative images of confocal microscopy of companion M6R treated cultures stained with specific anti-uPAR (red), α5β1 (green) and DAPI (blue). Experiments have been performed three times in triplicate with analogous results. The co-localization score is quantified by image J andreported within each picture as Manders' coefficient (MC). The shown pictures are representative of 20 different pictures for each experimental condition. Scale bar = 20 μm.

p-Akt(Thr308); 

PubMed: 27293997     


Vemurafenib reduced phosphorylated Akt in HUVEC. Cells were treated with vemurafenib for 4 h and processed for immunofluorescence staining with antibodies against p-AktThr308. Cell nuclei were stained with DAPI. Scale bar represents 50 μm. 

30611716 27293997
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]

Protocol

Kinase Assay:

[1]
+ Expand

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 Research:

[2]
+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[2]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 97 mg/mL (197.99 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O (suspension)
For best results, use promptly after mixing. 		5mg/mL

* 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 Information

Molecular Weight 489.92
Formula

C23H18ClF2N3O3S
CAS No. 918504-65-1
Storage powder
in solvent
Synonyms RO5185426

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03625141 Recruiting Metastatic Melanoma Hoffmann-La Roche December 13 2018 Phase 2
NCT03625141 Recruiting Metastatic Melanoma Hoffmann-La Roche December 13 2018 Phase 2
NCT03727763 Recruiting Colorectal Cancer Shanghai Changzheng Hospital October 8 2018 Phase 2
NCT03727763 Recruiting Colorectal Cancer Shanghai Changzheng Hospital October 8 2018 Phase 2

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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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.

selleck catalog

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID