All AbMole products are for research use only, cannot be used for human consumption.
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.
J Nucl Med. 2018 Nov 21.
MEK inhibition induces therapeutic iodine uptake in a murine model of anaplastic thyroid cancer.
PLX-4720 purchased from AbMole
BioRxiv. 2017; .
PIK3CAH1047R-induced paradoxical ERK activation results in resistance to BRAFV600E specific inhibitors in BRAFV600E PIK3CAH1047R double mutant thyroid tumors
PLX-4720 purchased from AbMole
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Source | Journal of Nuclear Medicine (2018 Nov). Figure 3. PLX-4720 (AbMole Bioscience Inc.) |
| Method | oral gavage | |
| Cell Lines | single mutant BRAFV600E mice | |
| Concentrations | 30 mg/kg | |
| Incubation Time | 10 days | |
| Results | The selective BRAFV600E inhibitor PLX-4720 did not increase Nis mRNA transcription, nor did the PI3K inhibitor GDC-0941 alone or in combination with PD-325901 or PLX-4720. |
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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 |
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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). |
| Cell Experiment | |
|---|---|
| Cell lines | A375, UACC-903, and BRAF wt cell lines |
| Preparation method | Cell proliferation assays Cellular proliferation was evaluated by MTT assay (AbMole) 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 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 |
| Molecular Weight | 413.83 |
| Formula | C17H14ClF2N3O3S |
| CAS Number | 918505-84-7 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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