All AbMole products are for research use only, cannot be used for human consumption.
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; AbMole) 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. |
| 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 |
| Related Raf Products |
|---|
| Sorafenib-d3
Sorafenib-d3 (Donafenib) is a deuterium-labeled Sorafenib, it is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively. |
| XL-281
XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC50s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. |
| B-Raf IN 2
B-Raf IN 2 is a potent and selective BRAF inhibitor. |
| Brimarafenibum
Brimarafenibum (Brimarafenib) is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor, wtih antineoplastic effect. |
| Belvarafenib TFA
Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. |
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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