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PLX4032

PLX4032 is a targeted cancer therapy that inhibits the BRAF V600E mutation, which is commonly found in melanoma and other cancer types.
This small-molecule inhibitor has shown promising results in clinical trials, demonstrating improved progression-free survival and response rates compared to standard treatments.
PubCompare.ai can help researchers optimize their PLX4032 studies by providing easy access to the latest protocols, pre-prints, and patents, while leveraging AI-driven comparisons to enhance reproducibility and accuracy.
This platform can improve research efficiency and lead to breakthroughs in the use of PLX4032 for personalized cancer treatment.
Ealiser access to the most up-to-date information and innovative analytical tools can accelerate the development of this important therapeutic option.

Most cited protocols related to «PLX4032»

1
Identifying Drug Sensitivity Modifiers
Cited 130 times
A375-Cas9 cells were infected in four biological replicates. Small molecules were added to puromycin-selected cells 7 days post-infection. Cells either received a media change or were passaged every two or three days over the course of the screen in complete media supplemented with 1% penicillin/streptomycin. Vemurafenib (PLX-4032, Selleckchem, S1267) was screened at a final concentration of 2 μM. Selumetinib (AZD-6244, Selleckchem, S1008) was screened at a final concentration of 200 nM. 6-thioguanine (Sigma A4660) was screened at a final concentration of 2 μg/mL. Etoposide (Sigma E1383) was screened at a final concentration of 1 μg/mL. Surviving cells were harvested after 14 days of small molecule treatment. For analysis, the log2-fold-change of each sgRNA was determined relative to control cells treated with DMSO.
Doench J.G., Fusi N., Sullender M., Hegde M., Vaimberg E.W., Donovan K.F., Smith I., Tothova Z., Wilen C., Orchard R., Virgin H.W., Listgarten J, & Root D.E. (2016). Optimized sgRNA design to maximize activity and minimize off-target effects of CRISPR-Cas9. Nature biotechnology, 34(2), 184-191.
Publication 2015
AZD 6244 Biopharmaceuticals Cells Etoposide Infection Penicillins PLX4032 Puromycin selumetinib Streptomycin Sulfoxide, Dimethyl Thioguanine Vemurafenib
2
Identifying Drug Sensitivity Modifiers
Cited 118 times
A375-Cas9 cells were infected in four biological replicates. Small molecules were added to puromycin-selected cells 7 days post-infection. Cells either received a media change or were passaged every two or three days over the course of the screen in complete media supplemented with 1% penicillin/streptomycin. Vemurafenib (PLX-4032, Selleckchem, S1267) was screened at a final concentration of 2 μM. Selumetinib (AZD-6244, Selleckchem, S1008) was screened at a final concentration of 200 nM. 6-thioguanine (Sigma A4660) was screened at a final concentration of 2 μg/mL. Etoposide (Sigma E1383) was screened at a final concentration of 1 μg/mL. Surviving cells were harvested after 14 days of small molecule treatment. For analysis, the log2-fold-change of each sgRNA was determined relative to control cells treated with DMSO.
Doench J.G., Fusi N., Sullender M., Hegde M., Vaimberg E.W., Donovan K.F., Smith I., Tothova Z., Wilen C., Orchard R., Virgin H.W., Listgarten J, & Root D.E. (2016). Optimized sgRNA design to maximize activity and minimize off-target effects of CRISPR-Cas9. Nature biotechnology, 34(2), 184-191.
Publication 2015
AZD 6244 Biopharmaceuticals Cells Etoposide Infection Penicillins PLX4032 Puromycin selumetinib Streptomycin Sulfoxide, Dimethyl Thioguanine Vemurafenib
3
Chemoresistant cancer cell line establishment
Cited 30 times
The N-myc-amplified neuroblastoma cell lines UKF-NB-2, UKF-NB-3, and UKF-NB-6 were established from stage 4 neuroblastoma patients.31 (link), 32 (link), 33 (link) The alveolar rhabdomyosarcoma cell line UKF-Rhb-1 was established from a bone marrow metastasis.11 (link) The melanoma cell lines Colo-679 and Mel-HO were obtained from the DSMZ (Braunschweig, Germany).
Parental chemosensitive cell lines were adapted to growth in the presence of anti-cancer drugs by continuous exposure of these cell lines to the increasing concentrations of these drugs as described before.31 (link), 32 (link)The following chemoresistant UKF-NB-3 sublines were derived from the resistant cancer cell line (RCCL) collection: UKF-NB-3rCDDP1000 (adapted to CDDP), UKF-NB-3rDAC8 (DAC), UKF-NB-3rDOX20 (DOX), UKF-NB-3rGEMCI10 (GEMCI), UKF-NB-3rIRINO800 (IRINO), UKF-NB-3rMEL400 (MEL), UKF-NB-3rOXALI2000 (OXALI), UKF-NB-3rPCL20 (PCL), UKF-NB-3rTOPO15 (TOPO), UKF-NB-3rVCR10 (VCR), and UKF-NB-3rVINOR20 (VINOR).
The following chemoresistant UKF-NB-2 sublines were derived from the RCCL collection: UKF-NB-2rCDDP1000, UKF-NB-2rDOX20, and UKF-NB-2rVCR10.
The following chemoresistant UKF-Rhb-1 sublines were derived from the RCCL collection: UKF-Rhb-1rCDDP1000 and UKF-Rhb-1rDOCE10 (DOCE), UKF-Rhb-1rDOX10, UKF-Rhb-1rGEMCI10, UKF-Rhb-1rIRINO200, UKF-Rhb-1rMEL400, UKF-Rhb-1rOXALI1000, and UKF-Rhb-1rVCR10Moreover, the following melanoma sub-lines were derived from the RCCL collection: Colo-679rVCR20, Colo-679rPLX403210 μM (PLX4032, vemurafenib), MelHOrVCR20, MelHOrCDDP1000, MelHOrDAC20, and MelHOrPLX403210 μM.
The corresponding IC50 values for the parental cells and their drug-resistant sublines are provided in Supplementary Table 4.
All cells were propagated in IMDM supplemented with 10% FBS, 100 IU/ml penicillin and 100 mg/ml streptomycin at 37 °C. Cells were routinely tested for mycoplasma contamination and authenticated by short tandem repeat profiling.
Standard molecular cloning techniques were used to generate lentiviral vectors based on Lentiviral Gene Ontology vector technology (see http://www.lentigo-vectors.de), and cell transduction was performed as described before.11 (link), 18 (link), 34 (link)
Michaelis M., Rothweiler F., Barth S., Cinatl J., van Rikxoort M., Löschmann N., Voges Y., Breitling R., von Deimling A., Rödel F., Weber K., Fehse B., Mack E., Stiewe T., Doerr H.W., Speidel D, & Cinatl J j.r. (2011). Adaptation of cancer cells from different entities to the MDM2 inhibitor nutlin-3 results in the emergence of p53-mutated multi-drug-resistant cancer cells. Cell Death & Disease, 2(12), e243-.
Publication 2011
Alveolar Epithelial Cells Alveolar Rhabdomyosarcoma Antineoplastic Agents Bone Marrow Cell Lines Cells Cisplatin Cloning Vectors Lentigo LINE-1 Elements Malignant Neoplasms Melanoma Mycoplasma Neoplasm Metastasis Neuroblastoma Parent Patients Penicillins Pharmaceutical Preparations PLX4032 Rhabdomyosarcoma Rhabdomyosarcoma 1 Short Tandem Repeat Streptomycin Topotecan Vemurafenib
4
Molecular Profiling of Melanoma Tumors
Cited 24 times
PLX4032 was synthesized using the general procedures previously described.6 (link) Expression and purification of B-RAF, structure determination, protein kinase activity measurements, and xenograft studies were carried out as previously described.6 (link) Clinical methods have also been recently described.5 (link) Melanoma patients were selected for study using previously described TaqMan® methodology.8 Semi-quantitative immunohistochemistry for pERK and Ki67 was performed on 5 μm-thick formalin-fixed paraffin-embedded tumor biopsies following H&E staining to determine pathologic diagnosis and tissue morphology and integrity. The degree of phospho-ERK staining in the nucleus and cytoplasm was interpreted semiquantitatively by assessing the intensity and extent of staining on the slides. For Ki67 staining, the percentage of positive cells was determined.
Bollag G., Hirth P., Tsai J., Zhang J., Ibrahim P.N., Cho H., Spevak W., Zhang C., Zhang Y., Habets G., Burton E.A., Wong B., Tsang G., West B.L., Powell B., Shellooe R., Marimuthu A., Nguyen H., Zhang K.Y., Artis D.R., Schlessinger J., Su F., Higgins B., Iyer R., D'Andrea K., Koehler A., Stumm M., Lin P.S., Lee R.J., Grippo J., Puzanov I., Kim K.B., Ribas A., McArthur G.A., Sosman J.A., Chapman P.B., Flaherty K.T., Xu X., Nathanson K.L, & Nolop K. (2010). Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 467(7315), 596-599.
Publication 2010
Biopsy Cell Nucleus Cytoplasm Diagnosis Formalin Heterografts Immunohistochemistry Melanoma Neoplasms Paraffin Embedding Patients PLX4032 Protein Kinases Tissues
5
Melanoma Cell Line Culture Protocol
Cited 22 times
PLX4032 (also known as RG7204 or RO5185426) was obtained under a materials transfer agreement (MTA) with Plexxikon (Berkeley, CA) and dissolved in DMSO (Fisher Scientific, Morristown, NJ) to a stock concentration of 10 mM. SKMEL28 was obtained from American Type Culture Collection (ATCC, Rockville, MD), and the remaining human melanoma cell lines (M series) were established from patient's biopsies under UCLA IRB approval #02-08-067. Cells were cultured in RPMI 1640 with L-glutamine (Mediatech Inc., Manassas, VA) containing 10% (unless noted, all percentages represent volume to volume) fetal bovine serum (FBS, Omega Scientific, Tarzana, CA) and 1% penicillin, streptomycin, and amphotericin (Omega Scientific). All cell lines were mycoplasma free when periodically tested using a Mycoalert assay (Lonza, Rockland, ME).
Søndergaard J.N., Nazarian R., Wang Q., Guo D., Hsueh T., Mok S., Sazegar H., MacConaill L.E., Barretina J.G., Kehoe S.M., Attar N., von Euw E., Zuckerman J.E., Chmielowski B., Comin-Anduix B., Koya R.C., Mischel P.S., Lo R.S, & Ribas A. (2010). Differential sensitivity of melanoma cell lines with BRAFV600E mutation to the specific Raf inhibitor PLX4032. Journal of Translational Medicine, 8, 39.
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Publication 2010
Amphotericin Biological Assay Biopsy Cell Lines Cells Glutamine Homo sapiens Melanoma Mycoplasma Penicillins PLX4032 RG7204 Streptomycin Sulfoxide, Dimethyl

Most recents protocols related to «PLX4032»

1
Migratory and Invasive Abilities of Cancer Cells
Not available on PMC !

Example 3

Cell migration is a highly-integrated and multi-step process that plays an important role in the progression of late-stage cancer. Cell invasion is involved in extracellular matrix degradation and proteolysis. In the study, wound healing assay and transwell invasion assay were used to examine migratory and invasive abilities of PDV cells, respectively, with or without PLX4032 stimulation. In invasion assay, PLX4032 promoted the invasive ability of PDV cells (FIG. 3). Further, in the presence or absence of PLX4032, KWM-EO, LM-EO and L+C treatment for 24 h reduced invaded cells on concentration-dependence.

In wound healing assay, 50 μg/mL KWM-EO, 50 μg/mL LM-EO and 40 μg/mL L+C reduced PDV cell migratory ability at 24 h treatment, and LM-EO had a better effect than the others (FIG. 4). On the other hand, 2 μM PLX4032 treatment strongly promoted cell migration of PDV cells within 24 h treatment, KWM-EO, LM-EO and L+C combination, similarly both EOs and compounds only, significantly suppressed PLX4032-stimulated migratory ability of PDV cells.

US11872260B2. Mint essential oils inhibit HRASQ61L mutant keratinocyte activity and prevent skin carcinogenesis (2024-01-16). ACADEMIA SINICA [TW]. Inventors: Lie-Fen Shyur [TW], Chih-Ting Chang [TW], Yuhsin Chen [TW].
Full text: Click here
Patent 2024
Biological Assay Cells Disease Progression Extracellular Matrix Mentha Migration, Cell Oils, Volatile PLX4032 Proteolysis Staging, Cancer
2
Inhibiting Colony Formation in PDV Cells
Not available on PMC !

Example 2

Colony formation assay was utilized to assess the capability of a single PDV cell growing into a colony with mint EOs of KWM or LM, L+C treatment or co-treated with PLX4032. The MEK inhibitor, AZD6244 was tested in parallel as a positive control. KWM-EO and LM-EO had significant effect on suppressing colony formation ability, but L+C combinational treatment had no effect (FIG. 2). Meanwhile, PLX4032 treatment significantly promoted PDV cell colony formation after treatment for six days. The colony formation ability of PDV cells stimulated by 0.5 μM PLX4032 was diminished by KWM-EO, LM-EO and L+C at tested concentrations. The EO from Lime Mint showed better inhibitory activity than that of KWM-EO. MEK inhibitor at 0.5 μM decreased clonogenic formation ability of PDV cells in the presence or absence of PLX4032.

US11872260B2. Mint essential oils inhibit HRASQ61L mutant keratinocyte activity and prevent skin carcinogenesis (2024-01-16). ACADEMIA SINICA [TW]. Inventors: Lie-Fen Shyur [TW], Chih-Ting Chang [TW], Yuhsin Chen [TW].
Full text: Click here
Patent 2024
Aftercare AZD 6244 Biological Assay calcium oxide Cardiac Arrest Cells Mentha Oils, Volatile PLX4032 Psychological Inhibition
3
Inhibition of MAPK Activation by Natural Compounds
Not available on PMC !

Example 6

It is well known that BRAF inhibitor PLX4032 can induce paradoxical MAPK activation and cause abnormal cell proliferation in RAS mutation cells. The expression level of MAPK signaling pathway related proteins in PDV cells was examined by western blotting (FIG. 7). PLX4032 at 0.5 μM promoted p-MEK and p-ERK protein expression at 6-24 h treatment. MEK inhibitor, AZD6244 reversed the up-regulation of p-ERK induced by PLX4032, while KWM-EO, LM-EO at 75 μg/mL and L+C at 60 μg/mL significantly abolished the p-MEK and p-ERK protein expression in PLX4032-stimulated PDV cells. KWM-EO, LM-EO and L+C treatment also decreased the expression of MEK but not ERK.

US11872260B2. Mint essential oils inhibit HRASQ61L mutant keratinocyte activity and prevent skin carcinogenesis (2024-01-16). ACADEMIA SINICA [TW]. Inventors: Lie-Fen Shyur [TW], Chih-Ting Chang [TW], Yuhsin Chen [TW].
Full text: Click here
Patent 2024
AZD 6244 BRAF protein, human Cell Proliferation Cells MAP Kinase Cascade Mutation OCA2 protein, human PLX4032 Proteins
4
Regulation of MAPK Signaling by Natural Compounds
Not available on PMC !

Example 11

Phosphorylation of ERK is an important hallmark of the MAPK signaling pathway that regulates cell proliferation, division, motility and death. The protein expression level of p-ERK in papillomas was further analyzed by IHC. Most of the p-ERK protein were expressed between the junction of subcutaneous layer and papillomas in DMBA/TPA-irritated mice skin and that can be down-regulated by KWM-EO, LM-EO and L+C treatments (FIG. 12). Previous study indicated that PLX4032 injection enhanced the activation of p-ERK on RAS gene mutated tissue that is also observed nicely in this study. The paradoxical activation of p-ERK was significantly blockaded by KWM-EO, LM-EO and L+C topical applications.

US11872260B2. Mint essential oils inhibit HRASQ61L mutant keratinocyte activity and prevent skin carcinogenesis (2024-01-16). ACADEMIA SINICA [TW]. Inventors: Lie-Fen Shyur [TW], Chih-Ting Chang [TW], Yuhsin Chen [TW].
Full text: Click here
Patent 2024
9,10-Dimethyl-1,2-benzanthracene Cell Proliferation Genes, ras MAP Kinase Cascade Mentha Motility, Cell Mus Oils, Volatile Papilloma Phosphorylation PLX4032 Proteins Skin Tissues
5
DMBA/TPA-Induced Mouse Skin Histopathology
Not available on PMC !

Example 10

H&E staining was performed to examine the histopathology of mouse skin tissues (FIG. 11). The typical skin architecture with epidermis, dermis, subcutis, muscle and hair follicles were observed in sham group mice. Topical application of DMBA/TPA resulted in an increase in epidermal thickness which is suggested to be abnormal proliferation and hyperplasia of the epidermis. The irregular thickness of the epidermis was attenuated by KWM-EO, LM-EO and L+C combination treatment. In DMBA-initiated and TPA-promoted skin, intraperitoneal injection of PLX4032 exacerbated the proliferation and hyperplasia of the epidermis. Mint EOs and major compound application also notably inhibited the unnatural thickness of the epidermis.

US11872260B2. Mint essential oils inhibit HRASQ61L mutant keratinocyte activity and prevent skin carcinogenesis (2024-01-16). ACADEMIA SINICA [TW]. Inventors: Lie-Fen Shyur [TW], Chih-Ting Chang [TW], Yuhsin Chen [TW].
Full text: Click here
Patent 2024
9,10-Dimethyl-1,2-benzanthracene Dermis Epidermis Hair Follicle Hyperplasia Injections, Intraperitoneal Mentha Mice, Laboratory Muscle Tissue PLX4032 Skin Subcutaneous Fat Tissues

Top products related to «PLX4032»

1
Plx4032 by Selleck Chemicals
Sourced in United States, Germany
PLX4032 is a laboratory compound used for research purposes. It functions as a selective inhibitor for the BRAF kinase enzyme. This compound is intended for use in scientific research and analysis, and its specific applications should be determined by the user.
2
Vemurafenib by Selleck Chemicals
Sourced in United States, Germany, France, China
Vemurafenib is a laboratory reagent used in research applications. It functions as a kinase inhibitor, specifically targeting the BRAF V600E mutation. This product is intended for research use only and its specific applications may vary depending on the research objectives.
3
Vemurafenib plx 4032 by Selleck Chemicals
Sourced in United States, Germany
Vemurafenib (PLX-4032) is a small-molecule, orally administered kinase inhibitor that targets the BRAF V600 mutation. It is a lab equipment product used for research purposes.
4
Dulbecco modified eagle medium (dmem) by Thermo Fisher Scientific
Sourced in United States, China, United Kingdom, Germany, France, Australia, Canada, Japan, Italy, Switzerland, Belgium, Austria, Spain, Israel, New Zealand, Ireland, Denmark, India, Poland, Sweden, Argentina, Netherlands, Brazil, Macao, Singapore, Sao Tome and Principe, Cameroon, Hong Kong, Portugal, Morocco, Hungary, Finland, Puerto Rico, Holy See (Vatican City State), Gabon, Bulgaria, Norway, Jamaica
DMEM (Dulbecco's Modified Eagle's Medium) is a cell culture medium formulated to support the growth and maintenance of a variety of cell types, including mammalian cells. It provides essential nutrients, amino acids, vitamins, and other components necessary for cell proliferation and survival in an in vitro environment.
5
Azd6244 by Selleck Chemicals
Sourced in United States, United Kingdom, China, Germany
AZD6244 is a small molecule inhibitor of the mitogen-activated protein kinase (MAPK) signaling pathway. It specifically targets the MEK enzyme, which is a key component of the MAPK cascade. AZD6244 is commonly used in laboratory research settings to study cell signaling and the role of the MAPK pathway in various biological processes.
6
Fetal bovine serum (fbs) by Thermo Fisher Scientific
Sourced in United States, China, United Kingdom, Germany, Australia, Japan, Canada, Italy, France, Switzerland, New Zealand, Brazil, Belgium, India, Spain, Israel, Austria, Poland, Ireland, Sweden, Macao, Netherlands, Denmark, Cameroon, Singapore, Portugal, Argentina, Holy See (Vatican City State), Morocco, Uruguay, Mexico, Thailand, Sao Tome and Principe, Hungary, Panama, Hong Kong, Norway, United Arab Emirates, Czechia, Russian Federation, Chile, Moldova, Republic of, Gabon, Palestine, State of, Saudi Arabia, Senegal
Fetal Bovine Serum (FBS) is a cell culture supplement derived from the blood of bovine fetuses. FBS provides a source of proteins, growth factors, and other components that support the growth and maintenance of various cell types in in vitro cell culture applications.
7
Dimethyl sulfoxide (dmso) by Merck Group
Sourced in United States, Germany, United Kingdom, China, Italy, Sao Tome and Principe, France, Macao, India, Canada, Switzerland, Japan, Australia, Spain, Poland, Belgium, Brazil, Czechia, Portugal, Austria, Denmark, Israel, Sweden, Ireland, Hungary, Mexico, Netherlands, Singapore, Indonesia, Slovakia, Cameroon, Norway, Thailand, Chile, Finland, Malaysia, Latvia, New Zealand, Hong Kong, Pakistan, Uruguay, Bangladesh
DMSO is a versatile organic solvent commonly used in laboratory settings. It has a high boiling point, low viscosity, and the ability to dissolve a wide range of polar and non-polar compounds. DMSO's core function is as a solvent, allowing for the effective dissolution and handling of various chemical substances during research and experimentation.
8
Penicillin streptomycin by Thermo Fisher Scientific
Sourced in United States, Germany, United Kingdom, China, Canada, France, Japan, Australia, Switzerland, Israel, Italy, Belgium, Austria, Spain, Gabon, Ireland, New Zealand, Sweden, Netherlands, Denmark, Brazil, Macao, India, Singapore, Poland, Argentina, Cameroon, Uruguay, Morocco, Panama, Colombia, Holy See (Vatican City State), Hungary, Norway, Portugal, Mexico, Thailand, Palestine, State of, Finland, Moldova, Republic of, Jamaica, Czechia
Penicillin/streptomycin is a commonly used antibiotic solution for cell culture applications. It contains a combination of penicillin and streptomycin, which are broad-spectrum antibiotics that inhibit the growth of both Gram-positive and Gram-negative bacteria.
9
Trametinib by Selleck Chemicals
Sourced in United States, Germany, United Kingdom, France, China, Italy
Trametinib is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) enzymes 1 and 2. It is a white to almost white crystalline powder that is used in various biomedical research applications.
10
Gsk1120212 by Selleck Chemicals
Sourced in United States, China, Germany
The GSK1120212 is a laboratory equipment product. It is a high-performance liquid chromatography (HPLC) instrument used for the separation, identification, and quantification of chemical compounds in complex mixtures. The GSK1120212 employs advanced chromatographic techniques to provide accurate and reliable analytical results for various research and development applications.

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