| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
SRMS (IC50 = 18 nM); ACK1 (IC50 = 19 nM); B-Raf (V600E) (IC50 = 48 nM); MAP4K5 (KHS1) (IC50 = 51 nM); C-Raf (IC50 = 48 nM)
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| ln Vitro |
Vemurafenib (PLX4032) specifically inhibits the RAF/MEK/ERK pathway in BRAF mutant cells[1]. In 17 melanoma cell lines, RG7204 is a potent inhibitor of proliferation in those that express RAFV600E but not BRAFWT. High concentrations of vemurafenib (RG7204) cause MEK and ERK phosphorylation in CHL-1 cells[2]. Resistance to PLX4032 can be brought on by EGFR expression in melanoma cells that is ectopically expressed[3].
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| ln Vivo |
Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) inhibits tumor growth in a dose-dependent manner, with higher exposures leading to tumor regression in xenografts harboring the BRAF mutation[1]. In mice bearing LOX tumor xenografts, RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and causes tumor regression[2].
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| Cell Assay |
Briefly, cells are plated in 96-well microtiter plates with a volume of 180 μL at a density of 1,000 to 5,000 cells per well. Vemurafenib (RG7204) is prepared for the assay in media containing 1% DMSO at 10 times the final assay concentration. 20 μL of the appropriate dilution are added to plates in duplicate twenty-four hours after cell plating. Six days after the cells are plated, the plates are tested for proliferation in accordance with the procedure.
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| Animal Protocol |
Athymic nude mice have a lifespan of 13 to 14 weeks and weigh between 23 and 25 g. 2×106 cells in 0.2 mL of PBS are injected subcutaneously into the right lateral flank for the LOX xenografts. In an aqueous vehicle containing 2% Klucel LF and pH 4-adjusted with diluted HCl, vemurafenib (RG7204), formulated as MBP, is suspended at the required concentration as needed for each dose group. There are 250-mg capsules of NSC 362856. Opened capsules are collected into a single bulk supply. NSC 362856 is first dissolved in 100% DMSO, then the DMSO is diluted with saline to create a final milky white suspension in 10% DMSO/90% saline (pH 3.4), which is the stock dosing material.
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| References |
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| Molecular Formula |
C23H18CLF2N3O3S
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|---|---|
| Molecular Weight |
489.92
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| Exact Mass |
489.07
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| Elemental Analysis |
C, 56.39; H, 3.70; Cl, 7.24; F, 7.76; N, 8.58; O, 9.80; S, 6.54
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| CAS # |
918504-65-1
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| Related CAS # |
Vemurafenib-d5;1365986-90-8;Vemurafenib-d7;1365986-73-7
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| Appearance |
White to off-white crystalline solid
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| SMILES |
CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(C=C4)Cl)F
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| InChi Key |
GPXBXXGIAQBQNI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
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| Chemical Name |
N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide
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| Synonyms |
Vemurafenib; RO5185426; RG7204; PLX 4032; RG 7204; RO 5185426; RG-7204; RO5185426; PLX4032; PLX-4032; trade name: Zelboraf
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 4% DMSO +30% PEG 300 +5% Tween 80 +ddH2O: 5mg/mL Solubility in Formulation 4: 3.33 mg/mL (6.80 mM) in 1.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0411 mL | 10.2057 mL | 20.4115 mL | |
| 5 mM | 0.4082 mL | 2.0411 mL | 4.0823 mL | |
| 10 mM | 0.2041 mL | 1.0206 mL | 2.0411 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02304809 | Active Recruiting |
Drug: Vemurafenib | Solid Tumors Hematologic Cancers |
UNICANCER | October 13, 2014 | Phase 2 |
| NCT01711632 | Active Recruiting |
Drug: Vemurafenib | Hairy Cell Leukemia | Memorial Sloan Kettering Cancer Center |
October 2012 | Phase 2 |
| NCT02036086 | Active Recruiting |
Drug: Vemurafenib Drug: Cobimetinib |
Melanoma | Sunnybrook Health Sciences Centre | August 2015 | Phase 2 |
| NCT03410875 | Active Recruiting |
Drug: Vemurafenib Drug: Obinutuzumab |
Leukemia Hairy Cell Leukemia |
Memorial Sloan Kettering Cancer Center |
February 9, 2018 | Phase 2 |
| NCT02721459 | Active Recruiting |
Drug: XL888 Drug: Vemurafenib |
Melanoma Skin Cancer |
H. Lee Moffitt Cancer Center and Research Institute |
September 7, 2016 | Phase 1 |
Mol Cancer Ther; 15(8); 1859–69, 2016 |
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