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Src I1

SRC kinase inhibitor
Catalog No. S19-901


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Catalog No. Pack Size Price (USD)
S19-901-05 5 mg $83
S19-901-25 25 mg $347
S19-901-BULK BULK Contact Us  


Overview:

Potent, competitive dual site (ATP- and substrate-binding domains) Src and Lck inhibitor (IC50 = 44 and 88 nM respectively). Also inhibits VEGFR2 and c-fms at higher concentrations (IC50 = 0.32 and 30 uM respectively).

References:


1. Tian et al. Biochem. 2001 40:7084

2. J Bain et al. Biochem. J. 2007 408:297


CAS Registry Number:

179248-59-0


Molecular Formula:

C22H19N3O3


Appearance:

White solid


Melting Point:

243-245oC


Molecular Weight:

373.4


Purity:

≥98% (TLC; 5% CH3OH in CH2Cl2; Rf=0.43); NMR (Conforms)


Solubilization:

Soluble in DMSO (15 mg/ml); Ethanol (nil)


Aliases:

6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine


Storage and Stability:

Store desiccated as supplied at ambient temperature for up to 3 years. Store solutions at -20oC for up to 3 months.


Molecular Structure:



Product Datasheets



 Keller N et al., Studies of the molecular mechanism of caspase-8 activation by solution NMR Cell Death and Differentiation April 2010 10.1038/cdd.2009.155

 Patela Priyank et al., Brk/Protein Tyrosine Kinase 6 Phosphorylates p27KIP1, Regulating the Activity of Cyclin D?Cyclin-Dependent Kinase 4 Molecular and Cellular Biology January 2015 10.1128/MCB.01206-14

 Gupta Shalini et al., Kinase-Actuated Immunoaggregation of Peptide-Conjugated Gold Nanoparticles Small June 2010 10.1002/smll.201000099

 Huang Yongqi et al., The Activity and Stability of the Intrinsically Disordered Cip/Kip Protein Family AreRegulated by Non-Receptor Tyrosine Kinases Journal of Molecular Biology January 2015 10.1016/j.jmb.2014.11.011

 Jun Cho Hee et al., EphrinB1 Interacts with CNK1 and Promotes Cell Migration through c-Jun N-terminal Kinase (JNK) Activation Journal of Biological Chemistry May 2014 10.1074/jbc.M114.558809

 Nama Sangkil et al., Novel synthetic derivatives of the natural product berbamine inhibit Jak2/Stat3 signaling and induce apoptosis of human melanoma cells Molecular Oncology October 2012 10.1016/j.molonc.2012.05.002

 E. Salhia Hussam et al., Cardiac troponin I tyrosine 26 phosphorylation decreases myofilament Ca 2+ sensitivity and accelerates deactivation Journal of Molecular and Cellular Cardiology September 2014 10.1016/j.yjmcc.2014.09.013

 Zhou Xi et al., The CHMP4b- and Src-docking sites in the Bro1 domain are autoinhibited in the native state of Alix Biochemical Journal March 2009 10.1042/BJ20081388

 Ghadiali JE et al., Protein Kinase-Actuated Resonance Energy Transfer in Quantum Dot-Peptide Conjugates ACS Nano July 2010 10.1021/nn101293s

 Beebe Kristin et al., Post-translational modification and conformational state of Heat Shock Protein 90 differentially affect binding of chemically diverse small molecule inhibitors Oncotarget July 2013 10.18632/oncotarget.1099

 Y Jin et al., Src drives the Warburg effect and therapy resistance by inactivating pyruvate dehydrogenase through tyrosine-289 phosphorylation. Oncotarget May 2016 10.18632/oncotarget.7159

 Figel Dwyer Sheila et al., Identification of Novel Focal Adhesion Kinase Substrates: Role for FAK in NFKB Signaling International Journal of Biological Sciences February 2015 10.7150/ijbs.10273

 Kosten Jonas et al., Efficient Modification of Alpha-Synuclein Serine 129 by Protein Kinase CK1 Requires Phosphorylation of Tyrosine 125 as a Priming Event ACS Chemical Neuroscience October 2014 10.1021/cn5002254

 Martic? Sanela et al., Electrochemical investigations into Tau protein phosphorylations Analyst March 2012 10.1039/c2an35097a

 Martica Sanela et al., Probing copper/tau protein interactions electrochemically Analytical Biochemistry November 2013 10.1016/j.ab.2013.07.015


RESEARCH AREAS

Angiogenesis, Apoptosis/Autophagy, Cancer, Cytoplasmic Tyrosine Kinases, ERK/MAPK Pathway, Inflammation, Invasion/Metastasis, JAK/STAT Pathway



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