Art. -Nr.: HY-51424

PLX-4720

17 Cited Publications

Kundenbewertung

Based on 17 publication(s) in Google Scholar

PLX-4720 is a potent and selective inhibitor of B-Raf^V600E with IC₅₀ of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf^V600E than wild-type B-Raf.

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Reinheit: 99.90%
CAS. Nr.: 918505-84-7
Formel: C₁₇H₁₄ClF₂N₃O₃S
Molecular Weight:413.83

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PLX-4720 Chemical Structure

CAS. Nr.: 918505-84-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

B-Raf^V600E

13 nM (IC₅₀)

B-Raf

160 nM (IC₅₀)

BRK

130 nM (IC₅₀)

FRK

1300 nM (IC₅₀)

Csk

1500 nM (IC₅₀)

Src

1700 nM (IC₅₀)

FAK

1700 nM (IC₅₀)

FGFR

1900 nM (IC₅₀)

KDR

2300 nM (IC₅₀)

HGK

2800 nM (IC₅₀)

CSF1R

3300 nM (IC₅₀)

Aurora A

3400 nM (IC₅₀)

Alle Raf Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
451Lu	IC₅₀	0.062 μM Compound: PLX-4720	Antiproliferative activity against human SB-590885-sensitive 451Lu cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Antiproliferative activity against human SB-590885-sensitive 451Lu cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 31784187]
A-375	GI₅₀	0.5 μM Compound: PLX4720	Antiproliferative activity against human A-375 cells harboring B-Raf V600E mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human A-375 cells harboring B-Raf V600E mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
A-375	IC₅₀	0.046 μM Compound: 17, PLX4720	Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK	[PMID: 22808911]
A-375	IC₅₀	0.5 μM Compound: 123; PLX-4720	Antiproliferative activity against human A-375 cells by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human A-375 cells by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 32798788]
A-375	IC₅₀	0.5 μM Compound: 17, PLX4720	Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras	[PMID: 22808911]
A-375	IC₅₀	500 nM Compound: 4; PLX-4720	Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay	[PMID: 29461827]
Calu-6	GI₅₀	26 μM Compound: PLX4720	Antiproliferative activity against human Calu-6 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Calu-6 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
COLO 205	GI₅₀	0.31 μM Compound: PLX4720	Antiproliferative activity against human COLO 205 cells harboring B-Raf V600E mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human COLO 205 cells harboring B-Raf V600E mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
COLO 205	IC₅₀	0.31 μM Compound: 123; PLX-4720	Antiproliferative activity against human COLO 205 cells by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human COLO 205 cells by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 32798788]
COLO-829	GI₅₀	1.7 μM Compound: PLX4720	Antiproliferative activity against human COLO-829 cells harboring B-Raf V600E mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human COLO-829 cells harboring B-Raf V600E mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
COLO-829	IC₅₀	1.7 μM Compound: 123; PLX-4720	Antiproliferative activity against human COLO-829 cells by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human COLO-829 cells by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 32798788]
HCT-116	GI₅₀	27 μM Compound: PLX4720	Antiproliferative activity against human HCT-116 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human HCT-116 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
HCT-116	IC₅₀	27 μM Compound: 17, PLX4720	Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant	[PMID: 22808911]
LoVo	GI₅₀	29 μM Compound: PLX4720	Antiproliferative activity against human LoVo cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human LoVo cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
NCI-H1299	GI₅₀	41 μM Compound: PLX4720	Antiproliferative activity against human NCI-H1299 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H1299 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
NCI-H460	GI₅₀	24 μM Compound: PLX4720	Antiproliferative activity against human NCI-H460 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H460 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
SK-MEL-2	GI₅₀	27 μM Compound: PLX4720	Antiproliferative activity against human SK-MEL-2 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-MEL-2 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
SK-MEL3	GI₅₀	27 μM Compound: PLX4720	Antiproliferative activity against human SK-MEL3 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-MEL3 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
SW-620	GI₅₀	13 μM Compound: PLX4720	Antiproliferative activity against human SW620 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SW620 cells harboring wildtype B-Raf assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
WM 266-4	GI₅₀	1.5 μM Compound: PLX4720	Antiproliferative activity against human WM266-4 cells harboring B-Raf V600D mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human WM266-4 cells harboring B-Raf V600D mutant assessed as growth inhibition incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 18287029]
WM 266-4	IC₅₀	1.5 μM Compound: 123; PLX-4720	Antiproliferative activity against human WM266-4 cells by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human WM266-4 cells by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 32798788]

In Vitro

PLX-4720 displays >10 times selectivity against wild type B-Raf, and >100 times selectivity over other kinases such as Frk, Src, Fak, FGFR, and Aurora A with IC₅₀ of 1.3-3.4 μM. PLX-4720 significantly inhibits the ERK phosphorylation in cell lines bearing B-Raf^V600E with IC₅₀ of 14-46 nM, but not the cells with wild-type B-Raf. PLX-4720 significantly inhibits the growth of tumor cell lines bearing the B-Raf^V600E oncogene, such as COLO205, A375, WM2664, and COLO829 with GI₅₀ of 0.31 μM, 0.50 μM, 1.5 μM, and 1.7 μM, respectively. In addition, PLX-4720 treatment at 1 μM induces cell cycle arrest and apoptosis exclusively in the B-Raf^V600E-positive 1205Lu cells, but not in the B-Raf wild-type C8161 cells^[1]. PLX-4720 treatment (10 μM) significantly induces > 14-fold expression of BIM in the PTEN⁺ cells, compared with the PTEN- cell lines (4-fold), giving an explanation of the resistance of PTEN- cells to PLX-4720-induced apoptosis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-Raf^V600E-dependent COLO205 tumor xenografts, without obvious adverse effects in mice even at dose of 1 g/kg. PLX-4720 at 100 mg/kg twice daily almost completely eliminates the 1205Lu xenografts bearing B-Raf^V600E, while has no activity against C8161 xenografts bearing wild-type B-Raf. The anti-tumor effects of PLX-4720 correlate with the blockade of MAPK pathway in those cells harboring the V600E mutation^[1]. PLX-4720 treatment at 30 mg/kg/day significant inhibits the tumor growth of 8505c xenografts by >90%, and dramatically decreases distant lung metastases^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 918505-84-7
Appearance Solid
Molecular Weight 413.83
Formel C₁₇H₁₄ClF₂N₃O₃S
Color White to off-white
SMILES

O=S(NC1=CC=C(C(C(C2=CNC3=NC=C(C=C23)Cl)=O)=C1F)F)(CCC)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (17)

All Cell Proliferation/Viability AssayWBIn Vivo Efficacy StudyCell Imaging/StainingIFIHCFlow Cytometry

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Journal Impact Factor

Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171
Cell Discov

A positive mechanobiological feedback loop controls bistable switching of cardiac fibroblast phenotype. [Abstract]

2022 Sep 6;8(1):84. PMID: 36068215

PLX-4720 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 6;8(1):84. [Abstract]

GsMTx4 (Piezo1 inhibitor) and the combination of PLX4720 (2 μM) and PF562271 (1 μM; inhibiting integrin β1) decreased the expression of α-SMA, nuclear translocation of YAP, and expression of CTGF, while increasedthe expression of phosphorylated (inactive) YAP in cardiac fibroblasts (CFs).

PLX-4720 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 6;8(1):84. [Abstract]

GsMTx4 (Piezo1 inhibitor) and the combination of PLX4720 (2 μM) and PF562271 (1 μM; inhibiting integrin β1) reduced activation of fibroblasts in conditions for which phenotypic reversal was otherwise impossible (St14).
Theranostics

SPI1-mediated MIR222HG transcription promotes proneural-to-mesenchymal transition of glioma stem cells and immunosuppressive polarization of macrophages. [Abstract]

2023 May 27;13(10):3310-3329. PMID: 37351164

PLX-4720 purchased from MedChemExpress. Usage Cited in: Theranostics. 2023 May 27;13(10):3310-3329. [Abstract]

CCK-8 assay of GSC20 and GSC267 cells treated with different concentrations of PLX-4720 (0-1000 μM) for 48 hours.

PLX-4720 purchased from MedChemExpress. Usage Cited in: Theranostics. 2023 May 27;13(10):3310-3329. [Abstract]

Comet assays of GSC267 cells treated with IR (6 Gy) and PLX-4720.

PLX-4720 purchased from MedChemExpress. Usage Cited in: Theranostics. 2023 May 27;13(10):3310-3329. [Abstract]

PLX-4720 and radiotherapy resulted in further increases in apoptosis and further G2/M arrest in GSCs.
J Clin Invest

Neuropilin-1 upregulation elicits adaptive resistance to oncogene-targeted therapies. [Abstract]

2018 Aug 31;128(9):3976-3990. PMID: 29953416

PLX-4720 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2018 Aug 31;128(9):3976-3990. [Abstract]

NRP1 expression assessed by immunoblotting in parental and PLX-4720-resistant A375 cells transfected with pre-miRNA-338 (or mock transfected).
Adv Healthc Mater

Biofabrication and Monitoring of a 3D Printed Skin Model for Melanoma. [Abstract]

2024 Jul 11:e2401136. PMID: 38992996
Proc Natl Acad Sci U S A

Activation of the NLRP1 inflammasome in human keratinocytes by the dsDNA mimetic poly(dA:dT). [Abstract]

2023 Jan 31;120(5):e2213777120. PMID: 36693106
EMBO Mol Med

Portimine A toxin causes skin inflammation through ZAKα-dependent NLRP1 inflammasome activation. [Abstract]

2025 Mar;17(3):535-562. PMID: 39948420
J Med Chem

Systems Biology-Based Drug Repositioning Identifies Extracellular Matrix Module as a Therapeutic Target in Lung Squamous Cell Carcinoma. [Abstract]

2025 Oct 17. PMID: 41105954
Mol Syst Biol

Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis. [Abstract]

2015 Mar 26;11(3):797. PMID: 25814555
Cell Mol Life Sci

Targeting NG2 relieves the resistance of BRAF-mutant thyroid cancer cells to BRAF inhibitors. [Abstract]

2024 May 25;81(1):238. PMID: 38795180

PLX-4720 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 May 25;81(1):238. [Abstract]

PLX-4720 (20 mg/kg；PO; daily for 2 weeks) significantly delayed the growth of NG2-knockout tumors (NG2-KO) compared with DMSO treatment in Ng2 ^flox/flox C57Bl/6 mouse (NG2-knockout 8505 C cells).

PLX-4720 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 May 25;81(1):238. [Abstract]

PLX-4720 (20 mg/kg; PO; daily for 2 weeks) caused a significant decrease in the number of Ki67-positive cells and the levels of p-ERK and p-AKTT³⁰⁸ in NG2-knockout tumors, but not in control tumors in Ng2 ^flox/flox C57Bl/6 mouse (NG2-knockout 8505 C cells).

PLX-4720 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 May 25;81(1):238. [Abstract]

PLX-4720 (2 μM; 0, 1, 3, 6, 12, 24 h) suppressed the rebound of p-ERK and p-AKTT³⁰⁸ in NG2-knockout 8505 C cells.
ACS Chem Biol

A Chemical Probe Strategy for Interrogating Inhibitor Selectivity Across the MEK Kinase Family. [Abstract]

2017 May 19;12(5):1245-1256. PMID: 28263556
Biochem Genet

The Role of Coagulation-Related Genes in Glioblastoma: A Comprehensive Analysis of the Tumor Microenvironment, Prognosis, and Treatment. [Abstract]

2025 Mar 20. PMID: 40113719
bioRxiv

2026 Jan 25.
bioRxiv

2025 Sep 5.
bioRxiv

Dissecting Branch-Specific Unfolded Protein Response Activation in Drug-Tolerant BRAF-Mutant Melanoma using Data-Independent Acquisition Mass Spectrometry. [Abstract]

2025 Mar 24:2025.03.20.644425. PMID: 40196682
bioRxiv

CDDO-Methyl Ester Inhibits BRAF Inhibitor Resistance and Remodels the Myeloid Compartment in BRAF-mutant Melanoma. [Abstract]

2023 Aug 3:2023.08.01.551524. PMID: 37577680
Evid Based Complement Alternat Med

Inhibitory Effects of Euphorbia ebracteolata Hayata Extract ECB on Melanoma-Induced Hyperplasia of Blood Vessels in Zebrafish Embryos. [Abstract]

2021 Apr 26:2021:5543259. PMID: 33995546

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (241.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4165 mL

12.0823 mL

24.1645 mL

5 mM

0.4833 mL

2.4165 mL

4.8329 mL

10 mM

0.2416 mL

1.2082 mL

2.4165 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

For each enzyme (0.1 ng), 20-μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl₂, 1 mM DTT, 0.01% Tween-20, 100 nM biotin-MEK protein, various ATP concentrations, and increasing concentrations of PLX-4720 at room temperature. Reactions are stopped at 2, 5, 8, 10, 20, and 30 minutes with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, and 0.3% BSA. The stop solution also includes phospho-MEK Antibody, Streptavidin-coated Donor beads and Protein A Acceptor beads from the AlphaScreen Protein A Detection Kit. The antibody and beads are preincubated in stop solution in the dark at room temperature for 30 minutes. The final dilution of antibody is 1/2,000, and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour then are read on a PerkinElmer AlphaQuest reader.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Cells are treated with various concentrations PLX-4720 for 24, 48, and 72 hours. Cell proliferation is measured by using the CellTiter-Glo Luminescent Cell Viability Assay or MTT assay. For cell cycle analysis, supernatant and cells are collected, pelleted, and fixed with 70% ethanol. Before staining with propidium iodide (10 μg/mL), cells are incubated for 1 hour at 37°C in 0.5 mg/mL RNase I to rid samples of residual RNA contamination. Samples are then analyzed by using the EPICS XL apparatus. For the assessment of apoptosis, media and cells are harvested and pelleted before staining with annexin-FITC and propidium iodide. Samples are subsequently analyzed by using the EPICS XL apparatus.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Metastatic melanoma cells (2×10⁶) are s.c. injected into the flanks of SCID mice and allowed appr 2 weeks to reach 0.125 mm³ in volume. Subsequently, the animals receive either 100 mg/kg PLX4720 (oral gavage) or vehicle control twice daily for 15 days. Tumor volume is recorded every 72 h. The average tumor size for each respective group is normalized to the tumor volume at the first day of treatment. After 15 days of treatment, animals are killed and tumors are excised, fixed in formalin, paraffin-embedded, and analyzed by immunohistochemistry.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (396 KB)
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- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046. [Content Brief]

[2]. Paraiso KH, et al. PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression. Cancer Res, 2011, 71(7), 2750-2760. [Content Brief]

[3]. Nucera C, et al. B-Raf(V600E) and thrombospondin-1 promote thyroid cancer progression. Proc Natl Acad Sci U S A, 2010, 107(23), 10649-10654. [Content Brief]

[4]. Rizzolio S, et al. Neuropilin-1 upregulation elicits adaptive resistance to oncogene-targeted therapies. J Clin Invest. 2018 Aug 31;128(9):3976-3990. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4165 mL	12.0823 mL	24.1645 mL	60.4113 mL
	5 mM	0.4833 mL	2.4165 mL	4.8329 mL	12.0823 mL
	10 mM	0.2416 mL	1.2082 mL	2.4165 mL	6.0411 mL
	15 mM	0.1611 mL	0.8055 mL	1.6110 mL	4.0274 mL
	20 mM	0.1208 mL	0.6041 mL	1.2082 mL	3.0206 mL
	25 mM	0.0967 mL	0.4833 mL	0.9666 mL	2.4165 mL
	30 mM	0.0805 mL	0.4027 mL	0.8055 mL	2.0137 mL
	40 mM	0.0604 mL	0.3021 mL	0.6041 mL	1.5103 mL
	50 mM	0.0483 mL	0.2416 mL	0.4833 mL	1.2082 mL
	60 mM	0.0403 mL	0.2014 mL	0.4027 mL	1.0069 mL
	80 mM	0.0302 mL	0.1510 mL	0.3021 mL	0.7551 mL
	100 mM	0.0242 mL	0.1208 mL	0.2416 mL	0.6041 mL

Keywords

PLX-4720

17 Cited Publications

100 mg Angebot einholen

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PLX-4720

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PLX-4720

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Publications (17)

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PLX-4720 Related Classifications

HY-51424 Related Classifications