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 157 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 NUfuOGVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7FNVAxKM7:TR?= MX25OkBp NF\HZnZFVVOR MXnJR|UxRTR5IH7N M4fZNlE5PDV6MEWz
ARO NVjBWY16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOxNFAh|ryP NVPDb2pOQTZiaB?= MYnEUXNQ MX3JR|UxRTJyNTDuUS=> MWWxPFQ2QDB3Mx?=
NPA M{LCS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnC[llQOTByIN88US=> MlfwPVYhcA>? MlHESG1UVw>? MmXxTWM2OD1{NjDuUS=> NEHvTZkyQDR3OEC1Ny=>
TPCI NFTJfGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHy3ZnYyODBizszN M2Tob|k3KGh? MXTEUXNQ MkXRTWM2OD1zMD63O{DPxE1? MWixPFQ2QDB3Mx?=
A375 NXj4NYdmSXCxcITvd4l{KEG|c3H5 MkWwNVAh|ryP NGfKZodFVVOR MofDVJJwdW:2ZYOgZZBweHSxdHnjJIRm[XSq MXixPFQ2QDB3Mx?=
ARO M3PQS2Z2dmO2aX;uJGF{e2G7 NF7PTFUyOCEQvF2= M1zJZ|czKGh? NXnBeFA2TE2VTx?= MnTUTY5lfWOnczD0bIUhemWneIDy[ZN{cW:wIH;mJJRp\SCQSWOgdJVueA>? NF3oPWoyQDR3OEC1Ny=>
8505C (BRAF V600E/V600E) Mnj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2flN|k3KGh? MX;JR|UxRTV5IH7NJC=> NYmy[Ho3OjBzNEmxN|Y>
SW1736 (BRAF WT/V600E) M4TiNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnMdlA6PiCq NEP0T5ZKSzVyPUK5JI5O M1TXS|IxOTR7MUO2
BHT101 (BRAF WT/V600E) NUXZfINuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTQPVYhcA>? NWLFdFNCUUN3ME25O{BvVQ>? NHyxcWwzODF2OUGzOi=>
BCPAP (BRAF WT/V600E) M3Hqemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYq5OkBp M{T5N2lEPTB;N{igcm0> NVrPbIJkOjBzNEmxN|Y>
C643 (HRAS G13R)≥ 500 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f4Ulk3KGh? NH3QTXZKSzVyIPMJqUA2ODBibl2= MknUNlAyPDlzM{[=
HTH7 (NRAS Q61R) MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnp[4JkQTZiaB?= NXPsRpJzUUN3MPMJqUAyODByIH7N MUOyNFE1QTF|Nh?=
CAL62 (KRAS G12R) > 1000 > 1000 NF3rdllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\NVY1QQTZiaB?= NInTfJRKSzVyPjCxNFAxKG6P NVPNdZVjOjBzNEmxN|Y>
TPC-1 (RET/PTC1) NHTzOpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYO5OkBp M4LQc2lEPTEkibWxNFAxKG6P M3fUSVIxOTR7MUO2
PC MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfiVpE6PiCq MXXJR|UxRiBzMECwJI5O NED0WYozODF2OUGzOi=>
Calu-6 NGDMV5FHfW6ldHnvckBCe3OjeR?= NYfMTIZ1OeLCid88US=> M2KwdlEhcA>? M{XFNGROW09? MkDIRYN1cX[jdHXzJG1GUy:HUlugbY4h[2WubIOge4l1cCC5aXzkMZR6eGViQmLBSi=> MYGyNFE4QTdyNR?=
C4 NUPQO3BvTnWwY4Tpc44hSXO|YYm= MUSzJO69VQ>? NILPd3g1QCCq Mn63SG1UVw>? NFPpSphKdmO{ZXHz[ZMh[2:ubHHn[Y4he3mwdHjld4l{KGGwZDDk[YNz\WG|ZYOgTWwuQCCneIDy[ZN{cW:w NF\5UmYzPTl6OUWwOi=>
VMM12 MVvGeY5kfGmxbjDBd5NigQ>? MmT6N{DPxE1? M3zuNFQ5KGh? M4GyfGROW09? MmLBTY5kemWjc3XzJINwdGyjZ3XuJJN6dnSqZYPpd{BidmRiZHXjdoVie2W|IFnMMVkh\XiycnXzd4lwdg>? M4CzSlI2QTh7NUC2
SKMEL19 MWDGeY5kfGmxbjDBd5NigQ>? MVy2JO69VQ>? MlLYOFghcA>? M{jkOWROW09? NXTFb41nXHKrZ3fldpMhTVJic4Ty[ZN{ MWWyN|M3OjJ2MB?=
UKF-NB-3 (ABCB1) MUDGeY5kfGmxbjDBd5NigQ>? MVSxMlI2KML3TR?= NWmzNIJ{OiCq MoLNSG1UVw>? NWPHNJE4TW6qYX7j[ZMh[WOldX31cIF1cW:wIH;mJJRp\SCobIXvdoV{[2WwdDDBRmNDOSC|dXLzeJJifGVicnjv[IFucW6nIEGyNy=> MUWyOFc{PTd4Nh?=
UKF-NB-3 NYjxVW5LTnWwY4Tpc44hSXO|YYm= NEOzbWEyNjJ3INM1US=> MoHGNkBp MVXEUXNQ M1zhbXNq\26rZnnjZY51dHliYX\m[YN1eyCxbjDhZ4N2dXWuYYTpc44hd2ZidHjlJIZtfW:{ZYPj[Y51KEGEQ1KxJJN2[nO2cnH0[UBzcG:mYX3pcoUhOTJ| M1\lPVI1PzN3N{[2
A375 (BRAFV600E) NW[0UYxLTnWwY4Tpc44hSXO|YYm= M4KxUFghcA>? M{i0[mROW09? MX7JcoNz\WG|ZYOgbY51emGlZXzseYxieiCUT2OgZY5lKE6RIHzleoVteyB? NHXQPFIzPTN4M{[0OC=>

... 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03410875 Recruiting Drug: Vemurafenib|Drug: Obinutuzumab Hairy Cell Leukemia|Leukemia|Leukemia Hairy Cell Memorial Sloan Kettering Cancer Center|Dana-Farber Cancer Institute|Yale University February 9 2018 Phase 2
NCT03013491 Recruiting Drug: CX-072|Drug: ipilimumab|Drug: vemurafenib Solid Tumor|Lymphoma CytomX Therapeutics January 2017 Phase 1|Phase 2
NCT02441465 Completed Drug: Vemurafenib|Drug: 14C-Labeled Vemurafenib Malignant Melanoma Cancer Hoffmann-La Roche August 13 2015 Phase 1
NCT02427893 Withdrawn Drug: Cobimetinib|Drug: Vemurafenib Melanoma Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Genentech Inc. August 2015 Phase 3
NCT02036086 Active not recruiting Drug: Vemurafenib|Drug: Cobimetinib Melanoma Sunnybrook Health Sciences Centre August 2015 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

Raf Signaling Pathway Map

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    Sorafenib Tosylate : Approved by FDA for advanced renal cancer.

  • Newest Raf Inhibitor

    TAK-632 New : Potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID