Home Tools

Cart

Vemurafenib

Catalog No. T2382 CAS 918504-65-1

Synonyms: PLX4032, RO5185426, RG7204

Purity 99.65% Datasheet MSDS

Vemurafenib (PLX4032) is a novel and potent B-Raf (V600E) inhibitor (IC50: 31 nM).

Vemurafenib, CAS 918504-65-1

Pack Size	Availability	Price/USD
10 mg	In stock	50.00
50 mg	In stock	80.00
100 mg	In stock	112.00
200 mg	In stock	200.00
500 mg	In stock	340.00
1 mL * 10 mM (in DMSO)	In stock	50.00

Bulk Inquiry

Select Batch

Purity 97.69%

HNMR LCMS COA Datasheet MSDS

Purity 98.40%

HNMR HPLC COA Datasheet MSDS

Purity 99.65%

HNMR HPLC COA Datasheet MSDS

Biological Description

Chemical Properties

Storage & Solubility Information

Preparing Solutions

Description	Vemurafenib (PLX4032) is a novel and potent B-Raf (V600E) inhibitor (IC50: 31 nM).
Targets&IC50	ACK1 :ic50 19 nM (cell free), BLK :ic50 547nM, B-Raf :ic50 100nM, B-Raf (V600E) :ic50 31 nM (cell free), BRK :ic50 213nM, C-Raf :ic50 48nM, CSK :ic50 2.339μM, FGR :ic50 63nM, FRK (PTK5) :ic50 1.884μM, Lck :ic50 183nM, Lyn B :ic50 599nM, MAP4K5 (KHS1) :ic50 51nM, MNK2 :ic50 1.717μM, NEK11 :ic50 317nM, Src :ic50 2.389μM, SRMS :ic50 18 nM (cell free), WNK3 :ic50 877nM, Yes1 :ic50 604nM, c-Raf-1 :ic50 48 nM (cell free),
In vitro	Vemurafenib (PLX4032, RG7204) displays similar potency for B-RAFV600E (31nM) and c-RAF-1 (48nM) and selectivity against many other kinases, including wild type B-RAF (100nM) [1]. In 17 melanoma cell lines, RG7204 was a potent inhibitor of proliferation in those expressing BRAFV600E but not BRAFWT. RG7204 also potently inhibited proliferation of melanoma cell lines expressing other codons 600 BRAF mutations (V600D, V600K, and V600R) [2]. Melanoma cells were more sensitive to PLX4032 than CRC cells. The inhibition of EGFR does not significantly affect the proliferation of EGFR in WiDr cells. In contrast, suppression of EGFR in combination with PLX4032 caused a marked inhibition of proliferation in WiDr cells [3].
In vivo	In BRAFV600E-mutant xenograft, PLX4032 (6 or 8 mg/kg) demonstrated dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression [1]. In mice bearing Colo829 tumor xenografts, RG7204 at 100 mg/kg bid for 21 days showed greatly improved antitumor activity at the end of the study on day 38 after the tumor cell implant. There was complete tumor regression in all 10 mice treated with RG7204 by the end of the study [2]. In the dose-escalation cohort, among the 16 patients with melanoma whose tumors carried the V600E BRAF mutation and who were receiving 240 mg or more of PLX4032 twice daily, 10 had a partial response and 1 had a complete response [4].
Kinase Assay	Expression and purification of B-RAF, structure determination, and protein kinase activity measurements were carried out as previously described. To obtain co-crystals of B-RAFV600E with PLX4032, the protein solution was initially mixed with the compound dissolved in DMSO at a final compound concentration of 1 mM. This complex was co-crystallized by a sitting drop vapor diffusion experiment in which equal volumes of complex (at 10 mg/ml concentration) and reservoir solution (100mM BisTris at pH 6.0, 12.5% 2,5-hexanediol, and 12% PEG3350) were mixed and allowed to equilibrate against the reservoir at 4°C. The crystal was soaked in cryosolvent, followed by flash-freezing in liquid nitrogen. The data were collected at Beamline ALS831 with the wavelength of 1.11?. The Ramachandran plot from the refined structure shows that 94%, 5.6% and 0.4% residues are in the most favored, additional allowed and generously allowed regions, respectively. A summary of the crystallography statistics is included in Supplementary Table 3. COLO205 tumor xenograft studies (Molecular Imaging Research, Ann Arbor, MI) were carried out as previously described either using a conventional formulation (5%DMSO, 1% methylcellulose) or using the MBP formulation [1].
Cell Research	Cellular proliferation was evaluated by MTT 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 [2]. Cell lines: MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058 cells
Animal Research	All animal procedures were approved by the Ethical Commission of the Institute for Cancer Research and Treatment and by the Italian Ministry of Health. WiDr cells were injected subcutaneously into the right posterior flanks of 7-week-old immunodeficient NODSCID female mice (6 mice per group). Tumour formation was monitored twice a week, and tumour volume based on caliper measurements was calculated by the modified ellipsoidal formula: tumour volume = 1/2 length × width. When tumours reached a volume of approximately 200–250 mm^3, mice were randomly assigned to treatment with vehicle or drug(s) [3]. Animal Model: Mice (athymic nude) xenograft models of LOX, Colo829, and A375 cells

Synonyms	PLX4032 , RO5185426 , RG7204
Purity	97.69%
Molecular Weight	489.92
Formula	C23H18ClF2N3O3S
CAS No.	918504-65-1

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 90 mg/mL (183.7 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 5 mg/mL

Citations

References and Literature

1. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599. 2. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70(13), 5518-5527. 3. Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103. 4. Flaherty KT, et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med. 2010 Aug 26;363(9):809-19. 5. Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6(4):361-5.

Related compound libraries

This product is contained In the following compound libraries：

Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Stem cell Differentiation Compound Library Autophagy Compound Library Neuronal Signaling Compound Library MAPK Inhibitor Library Tyrosine kinase inhibitor library FDA-approved Drug Library Kinase Inhibitor Library Anti-cancer Approved drug Library Fluorochemical Library Angiogenesis related Compound Library

Related Products

Related compounds with same targets

NVP-AEW541 Sorafenib Sorafenib tosylate I-37 ZAP-180013 Plx-4032 B-Raf inhibitor 1 dihydrochloride Belvarafenib

Dose Conversion

Safe and effective drug dosing is necessary, regardless of its purpose of administration. Learn More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

mass of a compound required to prepare a solution of known volume and concentration
volume of solution required to dissolve a compound of known mass to a desired concentration
concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

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

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.

bottom

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 Products, and issues that need special attention for cell-based assays and animal experiments.

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.