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918505-84-7,MFCD14635203
Catalog No.:AA00GRRZ

918505-84-7 | PLX-4720

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1mg
99+%
in stock  
$7.00   $5.00
- +
5mg
99+%
in stock  
$14.00   $10.00
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10mg
99+%
in stock  
$17.00   $12.00
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25mg
99+%
in stock  
$23.00   $16.00
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50mg
99+%
in stock  
$28.00   $20.00
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250mg
95%
in stock  
$80.00   $56.00
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1g
99+%
in stock  
$154.00   $108.00
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00GRRZ
Chemical Name:
PLX-4720
CAS Number:
918505-84-7
Molecular Formula:
C17H14ClF2N3O3S
Molecular Weight:
413.8262
MDL Number:
MFCD14635203
SMILES:
CCCS(=O)(=O)Nc1ccc(c(c1F)C(=O)c1c[nH]c2c1cc(Cl)cn2)F
Properties
Properties
 
Form:
Solid  
MP:
230-233ºC  
Storage:
Keep in dry area;2-8℃;  

Computed Properties
 
Complexity:
648  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
27  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
6  
XLogP3:
3.3  

Downstream Synthesis Route

[1]Buck,JasonR.;Saleh,Sam;ImamUddin,Md.;Manning,H.Charles[TetrahedronLetters,2012,vol.53,#32,p.4161-4165]

918523-57-6   
N-(3-(5-chloro-1H-pyrrolo2,3-bpyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonoamide 

[1]Buck,JasonR.;Saleh,Sam;ImamUddin,Md.;Manning,H.Charles[TetrahedronLetters,2012,vol.53,#32,p.4161-4165]

[1]Buck,JasonR.;Saleh,Sam;ImamUddin,Md.;Manning,H.Charles[TetrahedronLetters,2012,vol.53,#32,p.4161-4165]

918505-84-7   
CASUnavailable 
  2230055-56-6 

[1]Kuttruff,ChristianA.;Haile,Margit;Kraml,Johannes;Tautermann,ChristoferS.[ChemMedChem,2018,vol.13,#10,p.983-987]

Literature

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

Title: Conformation-specific effects of Raf kinase inhibitors.

Journal: Journal of medicinal chemistry 20120913

Title: Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling.

Journal: The EMBO journal 20120530

Title: Role and therapeutic potential of PI3K-mTOR signaling in de novo resistance to BRAF inhibition.

Journal: Pigment cell & melanoma research 20120301

Title: Small molecule inhibitors of BRAF in clinical trials.

Journal: Bioorganic & medicinal chemistry letters 20120115

Title: Glutamatergic pathway targeting in melanoma: single-agent and combinatorial therapies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20111115

Title: Comprehensive analysis of kinase inhibitor selectivity.

Journal: Nature biotechnology 20111030

Title: B-Raf associates with and activates the NHE1 isoform of the Na+/H+ exchanger.

Journal: The Journal of biological chemistry 20110415

Title: Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer.

Journal: The oncologist 20110301

Title: MEK-independent survival of B-RAFV600E melanoma cells selected for resistance to apoptosis induced by the RAF inhibitor PLX4720.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110215

Title: Hyperactivation of MEK-ERK1/2 signaling and resistance to apoptosis induced by the oncogenic B-RAF inhibitor, PLX4720, in mutant N-RAS melanoma cells.

Journal: Oncogene 20110120

Title: Selective BRAFV600E inhibitor PLX4720, requires TRAIL assistance to overcome oncogenic PIK3CA resistance.

Journal: PloS one 20110101

Title: A switch in RND3-RHOA signaling is critical for melanoma cell invasion following mutant-BRAF inhibition.

Journal: Molecular cancer 20110101

Title: A simple protocol for using a LDH-based cytotoxicity assay to assess the effects of death and growth inhibition at the same time.

Journal: PloS one 20110101

Title: Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.

Journal: Chemistry & biology 20101124

Title: Apoptosis of human melanoma cells induced by inhibition of B-RAFV600E involves preferential splicing of bimS.

Journal: Cell death & disease 20100901

Title: Recovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibitor therapy.

Journal: British journal of cancer 20100608

Title: RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.

Journal: Nature 20100318

Title: RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF.

Journal: Nature 20100318

Title: Cytostatic activity of adenosine triphosphate-competitive kinase inhibitors in BRAF mutant thyroid carcinoma cells.

Journal: The Journal of clinical endocrinology and metabolism 20100101

Title: Effectively targeting BRAF in melanoma: a formidable challenge.

Journal: Pigment cell & melanoma research 20080801

Title: Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.

Journal: Proceedings of the National Academy of Sciences of the United States of America 20080226

Title: In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20030101

Title: 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.

Title: 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.

Title: 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.

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

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