Free shipping on all orders over $ 500

PLX4032

Cat. No. M1761
PLX4032 Structure
Synonym:

Vemurafenib, RG7204, RO5185426, Zelboraf

Size Price Availability Quantity
10mg USD 55 In stock
50mg USD 130 In stock
200mg USD 300 In stock
Bulk Inquiry?

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.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 489.92
Formula C23H18ClF2N3O3S
CAS Number 918504-65-1
Purity 100.00%
Solubility DMSO
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.

Related Raf Products
L-779450

L-779450 is a potent, ATP-competitive Raf kinase inhibitor (IC50 =10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck 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, respectively.

PF-04880594

PF-04880594 is a RAF inhibitor for BRAF/BRAFV599E and c-RAF with IC50 of 0.19 nM/0.13 nM and 0.39 nM, >100-fold selectivity over CSNK1, JNK2/3 and p38.

LGX818

LGX818 is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM.

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.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.