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.
Patent. CN118557576A 2024 Aug 30.
Patent. CN118557576A
Vemurafenib (PLX4032) purchased from AbMole
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
BioRxiv. 2017; .
PIK3CAH1047R-induced paradoxical ERK activation results in resistance to BRAFV600E specific inhibitors in BRAFV600E PIK3CAH1047R double mutant thyroid tumors
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 |
|---|
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GDC-0879 is a potent and selective B-Raf kinase inhibitor with an EC50 of 0.75 µM. |
| PLX-4720
PLX-4720 is a selective BRAFV600E inhibitor with the IC50 values of 160 nM and 130 nM for B-Raf and BRK respectively. |
| SB590885
SB590885 is a selective small-molecule inhibitor of the B-Raf kinase and Ki values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively. |
| ZM 336372
ZM 336372 is a potent, selective ATP-competitive inhibitor of c-Raf in vitro (IC50 = 70 nM for inhibition of human c-Raf). |
| Dabrafenib Mesylate
Dabrafenib (GSK2118436) is a selective, orally bioavailable inhibitor of Mutant B-raf (BRAF) protein kinase with potential antineoplastic activity. |
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