Vemurafenib (PLX4032) is a first-in-class, potent, selective inhibitor of B-Raf that inhibits RAFV600E and C-RAF-1 activity with IC50s of 31 nM and 48 nM, respectively.In addition, Vemurafenib induces autophagy.
Oncogene. 2021 Jun;40(24):4137-4150.
Targeting the p300/NONO axis sensitizes melanoma cells to BRAF inhibitors
Vemurafenib (PLX4032) purchased from AbMole
J Virol. 2020 Feb 14;94(5):e01791-19.
Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
Vemurafenib (PLX4032) purchased from AbMole
J Nucl Med. 2018 Nov 21.
MEK inhibition induces therapeutic iodine uptake in a murine model of anaplastic thyroid cancer.
Vemurafenib (PLX4032) purchased from AbMole
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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. |
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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. |
| 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 |
| Molecular Weight | 489.92 |
| Formula | C23H18ClF2N3O3S |
| CAS Number | 918504-65-1 |
| 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 |
| 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.
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Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM. |
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R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. |
| PROTAC RAF degrader 1
PROTAC RAF degrader 1 is a PROTAC RAF degrader. |
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