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.

Size Price Stock Quantity  
In DMSO USD 91 In stock
USD 70 In stock
USD 270 In stock
USD 770 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 315 Publications

Purity & Quality Control

Choose Selective Raf Inhibitors

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 NWXZNmdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofYNVAxKM7:TR?= MYm5OkBp MYfEUXNQ MUXJR|UxRTR5IH7N NWqweJRqOTh2NUiwOVM>
ARO MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn0NVAxKM7:TR?= MoLIPVYhcA>? MXPEUXNQ NXfWZotTUUN3ME2yNFUhdk1? M3zNS|E5PDV6MEWz
NPA MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DlNVExOCEQvF2= MUC5OkBp NGL6VFNFVVOR MkjHTWM2OD1{NjDuUS=> NYS1WGlzOTh2NUiwOVM>
TPCI M{jiUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17BUVExOCEQvF2= NVH1XpplQTZiaB?= MUHEUXNQ M{LwZ2lEPTB;MUCuO|ch|ryP M1;L[|E5PDV6MEWz
A375 MonsRZBweHSxc3nzJGF{e2G7 MYixNEDPxE1? MWTEUXNQ MlHNVJJwdW:2ZYOgZZBweHSxdHnjJIRm[XSq M2LVSVE5PDV6MEWz
ARO NFu5[FJHfW6ldHnvckBCe3OjeR?= NYnnfHZPOTBizszN M2HRS|czKGh? MmLqSG1UVw>? NIfvZVlKdmS3Y3XzJJRp\SC{ZXX4dJJme3Orb36gc4YhfGinIF7JV{BxfW2y MoX5NVg1PThyNUO=
8505C (BRAF V600E/V600E) NVHqd3RpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\6[FQ6PiCq NFnYfpNKSzVyPUW3JI5OKA>? M4[5c|IxOTR7MUO2
SW1736 (BRAF WT/V600E) NVvoUZZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV25OkBp MWfJR|UxRTJ7IH7N NUniWmo4OjBzNEmxN|Y>
BHT101 (BRAF WT/V600E) NVXtRZdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHKe2hyQTZiaB?= M2rweWlEPTB;OUegcm0> M3fPfFIxOTR7MUO2
BCPAP (BRAF WT/V600E) Moj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlO0PVYhcA>? MnPMTWM2OD15ODDuUS=> M3fhPVIxOTR7MUO2
C643 (HRAS G13R)≥ 500 M4f6Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfxPVYhcA>? M{LT[GlEPTBi4polJFUxOCCwTR?= MmXiNlAyPDlzM{[=
HTH7 (NRAS Q61R) NHf0ZWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYH0bHpHQTZiaB?= M4\QZmlEPTEkibWgNVAxOCCwTR?= NILuRWUzODF2OUGzOi=>
CAL62 (KRAS G12R) > 1000 > 1000 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr0XYs6PiCq M3iwXWlEPTB-IEGwNFAhdk1? Moe5NlAyPDlzM{[=
TPC-1 (RET/PTC1) MkHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;CR|k3KGh? NULtcIpDUUN3MPMJqVExODBibl2= MWeyNFE1QTF|Nh?=
PC M3\4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUS5OkBp MYLJR|UxRiBzMECwJI5O NULx[WxkOjBzNEmxN|Y>
Calu-6 NHf4[WJHfW6ldHnvckBCe3OjeR?= NEDFbHIy6oDLzszN M4qxZ|EhcA>? NXjoNlNpTE2VTx?= M1TLZ2FkfGm4YYTld{BOTUtxRWLLJIlvKGOnbHzzJJdqfGhid3ns[E11gXCnIFLSRWY> NYTyZnFVOjBzN{m3NFU>
C4 MnvYSpVv[3Srb36gRZN{[Xl? MYCzJO69VQ>? MWS0PEBp M4TCOGROW09? M{XRdmlv[3KnYYPld{Bkd2yuYXflckB{gW62aHXzbZMh[W6mIHTlZ5Jm[XOnczDJUE05KGW6cILld5Nqd25? M2qxSVI2QTh7NUC2
VMM12 NVLjXHhuTnWwY4Tpc44hSXO|YYm= NFW1dJE{KM7:TR?= NGLufno1QCCq MUTEUXNQ NFThUFRKdmO{ZXHz[ZMh[2:ubHHn[Y4he3mwdHjld4l{KGGwZDDk[YNz\WG|ZYOgTWwuQSCneIDy[ZN{cW:w NXHKPZV3OjV7OEm1NFY>
SKMEL19 Ml\LSpVv[3Srb36gRZN{[Xl? NGrSbG43KM7:TR?= MUC0PEBp MoHHSG1UVw>? M4H2NHRzcWepZYLzJGVTKHO2cnXzdy=> Mm\xNlM{PjJ{NEC=
UKF-NB-3 (ABCB1) NFXZb4lHfW6ldHnvckBCe3OjeR?= NVHuWotPOS5{NTFCuW0> NEfhVpMzKGh? NWHI[lZLTE2VTx?= MnL0SY5p[W6lZYOgZYNkfW23bHH0bY9vKG:oIITo[UBndHWxcnXzZ4VvfCCDQlPCNUB{fWK|dILheIUhemixZHHtbY5mKDF{Mx?= NHrLNYwzPDd|NUe2Oi=>
UKF-NB-3 NHfzU5hHfW6ldHnvckBCe3OjeR?= NX3sXZAzOS5{NTFCuW0> NHrNWIIzKGh? Mm\hSG1UVw>? NWLGWlZKW2mpbnnmbYNidnSueTDh[oZm[3S|IH;uJIFk[3WvdXzheIlwdiCxZjD0bIUh\my3b4Lld4NmdnRiQVLDRlEhe3Wkc4TyZZRmKHKqb3ThcYlv\SBzMkO= MofPNlQ4OzV5Nk[=
A375 (BRAFV600E) M1XjNGZ2dmO2aX;uJGF{e2G7 NF7KcHU5KGh? NILLXZZFVVOR NXXNfFRQUW6lcnXhd4V{KGmwdILhZ4VtdHWuYYKgVm9UKGGwZDDOU{Bt\X[nbIOg MYCyOVM3OzZ2NB?=

... 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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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

Raf Inhibitors with Unique Features

  • Selective Raf Inhibitors

    SB590885 : B-Raf-selective, Ki=0.16 nM.

  • Selective Raf Inhibitors

    ZM 336372 : C-Raf-selective, IC50=70 nM.

  • FDA-approved Raf Inhibitor

    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.

Related Raf Products

  • LY3009120 New

    LY03009120 is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.

  • Ravoxertinib (GDC-0994) New

    GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.

  • Ulixertinib (BVD-523, VRT752271) New

    Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

  • Dabrafenib (GSK2118436)

    Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

  • Sorafenib

    Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.

  • Sorafenib Tosylate

    Sorafenib Tosylate is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.

  • PLX-4720

    PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

  • TAK-632

    TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf in cell-free assays, respectively, showing less or no inhibition against other tested kinases.

  • GDC-0879

    GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.

  • GW5074

    GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted.

Tags: buy Vemurafenib (PLX4032, RG7204) | Vemurafenib (PLX4032, RG7204) supplier | purchase Vemurafenib (PLX4032, RG7204) | Vemurafenib (PLX4032, RG7204) cost | Vemurafenib (PLX4032, RG7204) manufacturer | order Vemurafenib (PLX4032, RG7204) | Vemurafenib (PLX4032, RG7204) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID