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Biological Activity for Saracatinib
Saracatinib is a potent and selective Src tyrosine kinase family inhibitor (IC50 = 4-10 nM). Inhibits Src, c-Yes, Fyn, Lyn, Blk, Fgr, and Lck. Exhibits selectivity over other tyrosine kinases (IC50 values are 30, 66 and 200 nM for v-Abl, EGFR and c-Kit, respectively). Suppresses invasion of HT1080 cells through a collagen matrix and inhibits metastasis in a murine model of bladder cancer. Inhibits the growth of prostate cancer cell lines. Also suppresses MERS-CoV replication at the early stage of replication (EC50 = 2.9 μM) and displays broad-spectrum activity against other human coronaviruses. Also blocks dengue virus RNA replication. Reverses memory deficit in a mouse AD model and rescues synapse density. Inhibits osteoclast activity, resorption and formation. Induces autophagy. Orally bioavailable.
Technical Data for Saracatinib
|Storage||Store at -20°C|
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 Saracatinib
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Saracatinib
The following data is based on the product molecular weight 542.03. 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|
|1 mM||1.84 mL||9.22 mL||18.45 mL|
|5 mM||0.37 mL||1.84 mL||3.69 mL|
|10 mM||0.18 mL||0.92 mL||1.84 mL|
|50 mM||0.04 mL||0.18 mL||0.37 mL|
References for Saracatinib
References are publications that support the biological activity of the product.
Hennequin et al (2006) N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. J.Med.Chem. 49 6465 PMID: 17064066
Green et al (2009) Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol.Oncol. 3 248 PMID: 19393585
De Wispelaere et al (2013) The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via Fyn kinase. J.Virol. 87 7367 PMID: 23616652
Kaufman et al (2015) Fyn inhibition rescues established memory and synapse loss in Alzheimer mice. Ann.Neurol. 77 953 PMID: 25707991
If you know of a relevant reference for Saracatinib, please let us know.
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Citations for Saracatinib
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Literature in this Area
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