Free shipping on all orders over $ 500

PLX-4720

Cat. No. M1774
PLX-4720 Structure
Synonym:

PLX4720

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 280 In stock
100mg USD 450 In stock
Bulk Inquiry?

Quality Control
Biological Activity

PLX-4720 is a selective BRAFV600E inhibitor with the IC50 values of 160 nM and 130 nM for B-Raf and BRK respectively. PLX-4720 shows remarkable selectivity for BRAF over a panel of 70 protein kinases due to its unusual binding mode, 40 and a similar selectivity is observed for its analogues. PLX-4720 has a BRAF IC50 of 13 nM, and in a panel of melanoma cell lines inhibits ERK activity only in those cell types that harbour the V600E mutation (pERK GI50 14–46 nM) whereas ERK remains unaffected in cells with WTBRAF.

Protocol
Cell Experiment
Cell lines A375, UACC-903, and BRAF wt cell lines
Preparation method Cell proliferation assays Cellular proliferation was evaluated by MTT assay (Sigma-Aldrich) following the manufacturer's instructions. Cells were plated in 96-well plates at 1,000 to 10,000 cells per well in 100 μL of media 24 hours after treatment and MTT signal was read at 72 hours after treatment. The IC50 and combination index (CI) by Chou–Talalay (16) were determined from the regression plot logarithm of the concentration versus effect using Calcusyn Software (Biosoft) v1.1. In addition, conservative isobolograms were used to show synergism and/or antagonism.
Concentrations 0~10µM
Incubation time 72h
Animal Experiment
Animal models Athymic nude mice Nu/Nu (Crl:NU-Foxn1nu) A375, A2058 (BRAF V600E-mutant), and Mel-Juso [BRAF wild-type (WT) and NRAS-mutant] xenograft tumor model
Formulation dimethyl sulfoxide (DMSO)
Dosages 50 mg/kg everyday
Administration intraperitoneal (i.p.) injections
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 413.83
Formula C17H14ClF2N3O3S
CAS Number 918505-84-7
Purity >99%
Solubility DMSO ≥81 mg/mL
Storage at -20°C
References

Differential inhibitory effects of two Raf-targeting drugs, sorafenib and PLX4720, on the growth of multidrug-resistant cells.
Eum KH, et al. Mol Cell Biochem. 2012 Sep 2. PMID: 22941213.

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.

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: PLX-4720, PLX4720 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.