918505-84-7 | PLX-4720

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$16.00	$11.00
5mg	95%	in stock	$23.00	$16.00
10mg	95%	in stock	$29.00	$20.00
25mg	95%	in stock	$36.00	$25.00
50mg	95%	in stock	$43.00	$30.00
100mg	95%	in stock	$55.00	$38.00
250mg	95%	in stock	$79.00	$55.00
1g	95%	in stock	$193.00	$135.00
5g	95%	in stock	$690.00	$483.00

Description

• Catalog Number: AH82395
• Chemical Name: PLX-4720
• CAS Number: 918505-84-7
• Molecular Formula: C17H14ClF2N3O3S
• Molecular Weight: 413.82616640000003
• MDL Number: MFCD14635203
• SMILES: CCCS(=O)(=O)Nc1ccc(c(c1F)C(=O)c1c[nH]c2c1cc(Cl)cn2)F

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

Literature

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

  Bioorganic & medicinal chemistry letters 20130801

• Conformation-specific effects of Raf kinase inhibitors.

  Journal of medicinal chemistry 20120913

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

  The EMBO journal 20120530

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

  Pigment cell & melanoma research 20120301

• Small molecule inhibitors of BRAF in clinical trials.

  Bioorganic & medicinal chemistry letters 20120115

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

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

• Comprehensive analysis of kinase inhibitor selectivity.

  Nature biotechnology 20111030

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

  The Journal of biological chemistry 20110415

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

  The oncologist 20110301

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

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

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

  Oncogene 20110120

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

  PloS one 20110101

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

  Molecular cancer 20110101

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

  PloS one 20110101

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

  Chemistry & biology 20101124

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

  Cell death & disease 20100901

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

  British journal of cancer 20100608

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

  Nature 20100318

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

  Nature 20100318

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

  The Journal of clinical endocrinology and metabolism 20100101

• Effectively targeting BRAF in melanoma: a formidable challenge.

  Pigment cell & melanoma research 20080801

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

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

• 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.

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