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PLX-4720

Cat. No. M1774
PLX-4720 Structure
Synonym:

PLX4720

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 70 In stock
50mg USD 220 In stock
100mg USD 350 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Customer Product Validations & Biological Datas
Source Oncotarget (2016). Figure 5. PLX-4720
Method proliferation assay
Cell Lines A375R cells
Concentrations 1 μM
Incubation Time 14 days
Results Importantly, in vitro derived PLX-4720 resistant A375R cells (cultured in the presence of 1μM PLX-4720) were growth inhibited by SB-431542
Source Oncotarget (2016). Figure 4. PLX-4720
Method proliferation assay
Cell Lines Colo829 and A375(M2) cells
Concentrations 62.5nM
Incubation Time 14 days
Results Importantly cotreatment of PLX-4720 treated mutant BRAF cells with SB-431542 (10μM) abolished the increase in cell growth caused by low dose PLX-4720 (Figure 4d and 4e).
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 >98%
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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PLX-4720, PLX4720 supplier, Raf, inhibitors

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