Science | Nature | Cell | View More
Natural Products
PLX-4720
PLX-4720
ChemFaces products have been cited in many studies from excellent and top scientific journals
Product Name PLX-4720
Price:
CAS No.: 918505-84-7
Catalog No.: CFN60059
Molecular Formula: C17H14ClF2N3O3S
Molecular Weight: 413.83 g/mol
Purity: >=98%
Type of Compound: Alkaloids
Physical Desc.: Powder
Source:
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download: COA    MSDS
Similar structural: Comparison
Guestbook:
Contact Us
Order & Inquiry & Tech Support

Tel: (0086)-27-84237683
Tech: service@chemfaces.com
Order: manager@chemfaces.com
Address: 176, CheCheng Eest Rd., WETDZ, Wuhan, Hubei 430056, PRC
How to Order
Orders via your E-mail:

1. Product number / Name / CAS No.
2. Delivery address
3. Ordering/billing address
4. Contact information
Order: manager@chemfaces.com
Delivery time
Delivery & Payment method

1. Usually delivery time: Next day delivery by 9:00 a.m. Order now

2. We accept: Wire transfer & Credit card & Paypal
Citing Use of our Products
* Packaging according to customer requirements(5mg, 10mg, 20mg and more). We shipped via FedEx, DHL, UPS, EMS and others courier.
According to end customer requirements, ChemFaces provide solvent format. This solvent format of product intended use: Signaling Inhibitors, Biological activities or Pharmacological activities.
Size /Price /Stock 10 mM * 1 mL in DMSO / Inquiry
Other Packaging *Packaging according to customer requirements(100uL/well, 200uL/well and more), and Container use Storage Tube With Screw Cap
Our products had been exported to the following research institutions and universities, And still growing.
  • Kyoto University (Japan)
  • Institute of Tropical Disease U... (Indonesia)
  • University of Dicle (Turkey)
  • Rio de Janeiro State University (Brazil)
  • Griffith University (Australia)
  • National Cancer Center Research... (Japan)
  • Osmania University (India)
  • University of Sao Paulo (Brazil)
  • Semmelweis Unicersity (Hungary)
  • Sri Sai Aditya Institute of Pha... (India)
  • Universiti Malaysia Pahang (Malaysia)
  • More...
Package
Featured Products
Isovitexin-2''-O-rhamnoside (2''-O...

Catalog No: CFN95314
CAS No: 72036-50-1
Price: $318/5mg
Pseudoprotodioscin

Catalog No: CFN90694
CAS No: 102115-79-7
Price: $138/20mg
Retronecine

Catalog No: CFN00322
CAS No: 480-85-3
Price: $ /
Hypaconitine

Catalog No: CFN99200
CAS No: 6900-87-4
Price: $98/20mg
Myrrhone

Catalog No: CFN91042
CAS No: 183551-83-9
Price: $388/5mg
6-Prenylnaringenin

Catalog No: CFN92017
CAS No: 68236-13-5
Price: $268/10 mg
Piperine

Catalog No: CFN99919
CAS No: 94-62-2
Price: $30/20mg
Juglanin

Catalog No: CFN96238
CAS No: 5041-67-8
Price: $318/5mg
Pectolinarin

Catalog No: CFN99727
CAS No: 28978-02-1
Price: $118/20mg
Astrasieversianin VII

Catalog No: CFN90648
CAS No: 86764-11-6
Price: $238/10mg
Related Screening Libraries
Size /Price /Stock 10 mM * 100 uL in DMSO / Inquiry / In-stock
10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries
Biological Activity
Description: PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
Targets: B-RafV600E
In vitro:
Cancer Res,2011 Apr 1;71(7):2750-60.
PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression.[Pubmed: 21317224]
This study addresses the role of PTEN loss in intrinsic resistance to the BRAF inhibitor PLX4720.
METHODS AND RESULTS:
Immunohistochemical staining of a tissue array covering all stages of melanocytic neoplasia (n = 192) revealed PTEN expression to be lost in >10% of all melanoma cases. Although PTEN expression status did not predict for sensitivity to the growth inhibitory effects of PLX4720, it was predictive for apoptosis, with only limited cell death observed in melanomas lacking PTEN expression (PTEN-). Mechanistically, PLX4720 was found to stimulate AKT signaling in the PTEN- but not the PTEN+ cell lines. Liquid chromatography multiple reaction monitoring mass spectrometry (LC-MRM) was performed to identify differences in apoptosis signaling between the two cell line groups. PLX4720 treatment significantly increased BIM expression in the PTEN+ (>14-fold) compared with the PTEN- cell lines (four-fold). A role for PTEN in the regulation of PLX4720-mediated BIM expression was confirmed by siRNA knockdown of PTEN and through reintroduction of PTEN into cells that were PTEN-. Further studies showed that siRNA knockdown of BIM significantly blunted the apoptotic response in PTEN+ melanoma cells. Dual treatment of PTEN- cells with PLX4720 and a PI3K inhibitor enhanced BIM expression at both the mRNA and protein level and increased the level of apoptosis through a mechanism involving AKT3 and the activation of FOXO3a.
CONCLUSIONS:
In conclusion, we have shown for the first time that loss of PTEN contributes to intrinsic BRAF inhibitor resistance via the suppression of BIM-mediated apoptosis.
In vivo:
Proc Natl Acad Sci U S A,2010 Jun 8;107(23):10649-54.
B-Raf(V600E) and thrombospondin-1 promote thyroid cancer progression.[Pubmed: 20498063]
Although B-Raf(V600E) is the most common somatic mutation in papillary thyroid carcinoma (PTC), how it induces tumor aggressiveness is not fully understood.
METHODS AND RESULTS:
Using gene set enrichment analysis and in vitro and in vivo functional studies, we identified and validated a B-Raf(V600E) gene set signature associated with tumor progression in PTCs. An independent cohort of B-Raf(V600E)-positive PTCs showed significantly higher expression levels of many extracellular matrix genes compared with controls. We performed extensive in vitro and in vivo validations on thrombospondin-1 (TSP-1), because it has been previously shown to be important in the regulation of tumor angiogenesis and metastasis and is present in abundance in tumor stroma. Knockdown of B-Raf(V600E) resulted in TSP-1 down-regulation and a reduction of adhesion and migration/invasion of human thyroid cancer cells. Knockdown of TSP-1 resulted in a similar phenotype. B-Raf(V600E) cells in which either B-Raf(V600E) or TSP-1 were knocked down were implanted orthotopically into the thyroids of immunocompromised mice, resulting in significant reduction in tumor size and fewer pulmonary metastases from the primary carcinoma as compared with the control cells. Treatment of orthotopic thyroid tumors, initiated 1 week after tumor cell implantation with PLX4720, an orally available selective inhibitor of B-Raf(V600E), caused a significant tumor growth delay and decreased distant metastases, without evidence of toxicity.
CONCLUSIONS:
In conclusion, B-Raf(V600E) plays an important role in PTC progression through genes (i.e., TSP-1) important in tumor invasion and metastasis. Testing of a patient's thyroid cancer for B-Raf(V600E) will yield important information about potential tumor aggressiveness and also allow for future use of targeted therapies with selective B-Raf(V600E) inhibitors, such as PLX4720.
PLX-4720 Description
Source:
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
ChemFaces New Products and Compounds
Apigenin 6,8-di-C-alpha-L-arabinop...

Catalog No: CFN95360
CAS No: 73140-47-3
Price: $318/10mg
Hainanic acid B

Catalog No: CFN95526
CAS No: 1637737-46-2
Price: $413/5mg
Ganoderic acid beta

Catalog No: CFN95537
CAS No: 217476-76-1
Price: $413/5mg
Polygalasaponin XXXV

Catalog No: CFN95176
CAS No: 184479-28-5
Price: $463/5mg
Kaempferol 3,5-O-diglucoside

Catalog No: CFN95487
CAS No: 205103-97-5
Price: $318/5mg
7-(4-Hydroxyphenyl)-1-phenyl-4-hep...

Catalog No: CFN95140
CAS No: 100667-52-5
Price: $318/5mg
Solafuranone

Catalog No: CFN95312
CAS No: 367965-50-2
Price: $318/5mg
Arisantetralone B

Catalog No: CFN95211
CAS No: 1161947-96-1
Price: $413/5mg
Recently, ChemFaces products have been cited in many studies from excellent and top scientific journals

Cell. 2018 Jan 11;172(1-2):249-261.e12.
doi: 10.1016/j.cell.2017.12.019.
IF=36.216(2019)

PMID: 29328914

Cell Metab. 2020 Mar 3;31(3):534-548.e5.
doi: 10.1016/j.cmet.2020.01.002.
IF=22.415(2019)

PMID: 32004475

Mol Cell. 2017 Nov 16;68(4):673-685.e6.
doi: 10.1016/j.molcel.2017.10.022.
IF=14.548(2019)

PMID: 29149595

ACS Nano. 2018 Apr 24;12(4): 3385-3396.
doi: 10.1021/acsnano.7b08969.
IF=13.903(2019)

PMID: 29553709

Nature Plants. 2016 Dec 22;3: 16206.
doi: 10.1038/nplants.2016.205.
IF=13.297(2019)

PMID: 28005066

Sci Adv. 2018 Oct 24;4(10): eaat6994.
doi: 10.1126/sciadv.aat6994.
IF=12.804(2019)

PMID: 30417089
Calculate Dilution Ratios(Only for Reference)
1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4165 mL 12.0823 mL 24.1645 mL 48.329 mL 60.4113 mL
5 mM 0.4833 mL 2.4165 mL 4.8329 mL 9.6658 mL 12.0823 mL
10 mM 0.2416 mL 1.2082 mL 2.4165 mL 4.8329 mL 6.0411 mL
50 mM 0.0483 mL 0.2416 mL 0.4833 mL 0.9666 mL 1.2082 mL
100 mM 0.0242 mL 0.1208 mL 0.2416 mL 0.4833 mL 0.6041 mL
* Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
Protocol
Cell Research:
Proc Natl Acad Sci U S A,2008 Feb 26;105(8):3041-6.
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.[Pubmed: 18287029]
Cell lines:COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, and C8161 cells
Concentrations: Dissolved in DMSO, final concentrations ~1 mM
Incubation Time:  24, 48, and 72 hoursBR/> Method:
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.
Animal Research:
Proc Natl Acad Sci U S A,2008 Feb 26;105(8):3041-6.
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.[Pubmed: 18287029]
Animal Models: Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
Dosages:5, 20, or 100 mg/kg
Administration: Oral gavage once or twice daily
Isovitexin-2''-O-rhamnoside (2''-O...

Catalog No: CFN95314
CAS No: 72036-50-1
Price: $318/5mg
Pseudoprotodioscin

Catalog No: CFN90694
CAS No: 102115-79-7
Price: $138/20mg
Retronecine

Catalog No: CFN00322
CAS No: 480-85-3
Price: $ /
Hypaconitine

Catalog No: CFN99200
CAS No: 6900-87-4
Price: $98/20mg
Myrrhone

Catalog No: CFN91042
CAS No: 183551-83-9
Price: $388/5mg
6-Prenylnaringenin

Catalog No: CFN92017
CAS No: 68236-13-5
Price: $268/10 mg
Piperine

Catalog No: CFN99919
CAS No: 94-62-2
Price: $30/20mg
Juglanin

Catalog No: CFN96238
CAS No: 5041-67-8
Price: $318/5mg
Pectolinarin

Catalog No: CFN99727
CAS No: 28978-02-1
Price: $118/20mg
Astrasieversianin VII

Catalog No: CFN90648
CAS No: 86764-11-6
Price: $238/10mg
Tags: buy PLX-4720 | PLX-4720 supplier | purchase PLX-4720 | PLX-4720 cost | PLX-4720 manufacturer | order PLX-4720 | PLX-4720 distributor