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Submit ReviewFAK Inhibitor 14
Description: Selective FAK inhibitor
Alternative Names: Y15,NSC 677249
Chemical Name: 1,2,4,5-Benzenetetramine tetrahydrochloride
Biological Activity for FAK Inhibitor 14
FAK Inhibitor 14 is a selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. FAK Inhibitor 14 prevents FAK autophosphorylation at Y397 (IC50 = 1 μM), promotes cell detachment and inhibits cell adhesion in vitro. FAK Inhibitor 14 exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo.
Compound Libraries for FAK Inhibitor 14
FAK Inhibitor 14 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for FAK Inhibitor 14
| M. Wt | 284.01 |
| Formula | C6H10N4.4HCl |
| Storage | Desiccate at RT |
| CAS Number | 4506-66-5 |
| PubChem ID | 78260 |
| InChI Key | BZDGCIJWPWHAOF-UHFFFAOYSA-N |
| Smiles | NC1=C(N)C=C(N)C(N)=C1.Cl.Cl.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for FAK Inhibitor 14
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 14.2 | 50 | |
| DMSO | 21.3 | 75 |
Preparing Stock Solutions for FAK Inhibitor 14
The following data is based on the product molecular weight 284.01. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.75 mM | 4.69 mL | 23.47 mL | 46.95 mL |
| 3.75 mM | 0.94 mL | 4.69 mL | 9.39 mL |
| 7.5 mM | 0.47 mL | 2.35 mL | 4.69 mL |
| 37.5 mM | 0.09 mL | 0.47 mL | 0.94 mL |
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Product Datasheets for FAK Inhibitor 14
References for FAK Inhibitor 14
References are publications that support the biological activity of the product.
Golubovskaya et al (2008) A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumour growth. J.Med.Chem. 51 7405 PMID: 18989950
Hochwald et al (2009) A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle 8 2435 PMID: 19571674
If you know of a relevant reference for FAK Inhibitor 14, please let us know.
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Keywords: FAK Inhibitor 14, FAK Inhibitor 14 supplier, Selective, FAK, inhibitors, inhibits, Focal, Adhesion, Kinases, Inhibitor14, Y15, NSC, 677249, Kinase, 3414, Tocris Bioscience
23 Citations for FAK Inhibitor 14
Citations are publications that use Tocris products. Selected citations for FAK Inhibitor 14 include:
Shih et al (2014) Astroglial-derived periostin promotes axonal regeneration after spinal cord injury. Auton Neurosci 34 2438 PMID: 24523534
Afrikanova et al (2011) Inhibitors of Src and focal adhesion kinase promote endocrine specification: impact on the derivation of β-cells from human pluripotent stem cells. J Biol Chem 286 36042 PMID: 21852242
Jia et al (2018) Fibroblast activation protein-α promotes the growth and migration of lung cancer cells via the PI3K and sonic hedgehog pathways. Int J Mol Med 41 275 PMID: 29115573
Bastounis et al (2018) Matrix stiffness modulates infection of endothelial cells by Listeria monocytogenes via expression of cell surface vimentin. Mol Biol Cell 29 1571 PMID: 29718765
Ni et al (2018) Plectin protects podocytes from adriamycin-induced apoptosis and F-actin cytoskeletal disruption through the integrin α6β4/FAK/p38 MAPK pathway. J Cell Mol Med 22 5450 PMID: 30187999
Barbelanne et al (2013) Pathogenic NPHP5 mutations impair protein interaction with Cep290, a prerequisite for ciliogenesis. Hum Mol Genet 22 2482 PMID: 23446637
Mendoza-Naranjo et al (2013) ERBB4 confers metastatic capacity in Ewing sarcoma. EMBO Mol Med 5 1019 PMID: 23681745
Malenczyk et al (2013) CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release. J Biol Chem 288 32685 PMID: 24089517
Keasey et al (2013) Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression. Cell Commun Signal 11 35 PMID: 23693126
Wiel et al (2013) Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis. Cell Death Dis 4 e855 PMID: 24113189
Daniel A et al (2012) Contractile equilibration of single cells to step changes in extracellular stiffness. Biophys J 102 443-51 PMID: 22325266
Jantaree et al (2017) Homodimers of vanillin and apocynin decrease the metastatic potential of human cancer cells by inhibiting the FAK/PI3K/Akt signaling pathway. J.Agric.Food Chem. 65 2299 PMID: 28248106
Tsai et al (2013) OE and tamox. induce cell migration through GPR30 and activation of focal adhesion kinase (FAK) in endometrial cancers with low or without nuclear estrogen receptor α (ERα). PLoS One 8 e72999 PMID: 24039841
Thakur et al (2015) Inhibition of STAT3, FAK and Src mediated signaling reduces cancer stem cell load, tumorigenic potential and metastasis in breast cancer. Sci Rep 5 10194 PMID: 25973915
McLane and Ligon (2015) Palladin mediates stiffness-induced fibroblast activation in the tumor microenvironment. Biophys J 109 249 PMID: 26200861
Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749 PMID: 20071540
An et al (2016) Netrin-1 suppresses the MEK/ERK pathway and ITGB4 in pancreatic cancer. Oncotarget 7 24719 PMID: 27034160
Visavadiya (2016) Integrin-FAK signaling rapidly and potently promotes mitochondrial function through STAT3. Cell Communication and Signaling 14 32 PMID: 27978828
Konrad et al (2020) Focal adhesion kinase confers pro-migratory and antiapoptotic properties and is a potential therapeutic target in Ewing sarcoma. Mol Oncol 14 248-260 PMID: 31811703
Theo et al (2019) Vitronectin from brain pericytes promotes adult forebrain neurogenesis by stimulating CNTF. Exp Neurol 312 20-32 PMID: 30408465
Rengarajan et al (2016) Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes. PLoS One 12 e1005603 PMID: 27152864
Gutiérrez et al (2015) RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice. J Neurosci 10 e0135005 PMID: 26247610
Webber et al (2015) Combination of heat shock protein 90 and focal adhesion kinase inhibitors synergistically inhibits the growth of non-small cell lung cancer cells. Oncoscience 2 765 PMID: 26501082
Do you know of a great paper that uses FAK Inhibitor 14 from Tocris? Please let us know.
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Mitochondrial bioenergetics measurements by reagent screen.
By
Anonymous on 03/15/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: mouse brain endothelioma cell line
10 μM
