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PLX4032

Cat. No. M1761
PLX4032 Structure
Synonym:

Vemurafenib, RG7204, RO5185426, Zelboraf

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 27  USD30 In stock
10mg USD 36  USD40 In stock
25mg USD 63  USD70 In stock
50mg USD 90  USD100 In stock
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Quality Control
Biological Activity

PLX4032, also known as Vemurafenib, RG7204, RO5185426 and Zelboraf, is a highly selective B-Raf enzyme inhibitor with an IC50 of 44 nM against V600E-mutant BRAF.

Product Citations
Customer Product Validations & Biological Datas
Source Cell Death Differ (2016). Figure 2. PLX4032
Method western blot
Cell Lines BRAF mutant melanoma cell lines
Concentrations 3 μM
Incubation Time 24 h
Results PLX4032-induced upregulation of BIM and PUMA occurred normally in the control sgRNA transduced cell lines.
Source Cell Death Differ (2016). Figure 1. PLX4032
Method flow cytometry
Cell Lines BRAFWT cells
Concentrations 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time 24 h
Results We found that PLX4032 induced significant dose-dependent apoptosis over a time course of 5 days in all BRAF mutant melanoma cell lines (M14, UACC257, Malme3M, SKMEL5 and UACC62), whereas the BRAFWT cells (CHL-1) were unaffected.
Protocol
Cell Experiment
Cell lines MDA-MB-435 cells line
Preparation method Cellular proliferation assays Cellular proliferation was evaluated by 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT; Sigma) 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 . The IC50 was determined from the regression of a plot of the logarithm of the concentration versus percent inhibition by XLfit (version 4.2; IDBS) using the Dose-Response One-Site Model (#205).
Concentrations 0~10µM
Incubation time 6 days
Animal Experiment
Animal models Colo829 and A375 xenografts
Formulation an aqueous vehicle containing 2% Klucel LF (Hydroxypropylcellulose; Aqualon) and adjusted to pH 4 with dilute HCl.
Dosages 100 mg/kg bid
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 489.92
Formula C23H18ClF2N3O3S
CAS Number 918504-65-1
Purity 99.34%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

BH3-only protein silencing contributes to acquired resistance to PLX4720 in human melanoma.
Shao Y et al. Cell Death Differ. 2012 Aug 3. PMID: 22858545.

Vemurafenib (RG67204, PLX4032): a potent, selective BRAF kinase inhibitor.
Patrawala S et al. Future Oncol. 2012 May;8(5):509-23. PMID: 22646766.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PLX4032, Vemurafenib, RG7204, RO5185426, Zelboraf supplier, Raf, inhibitors

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