Saracatinib

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Kaufman Fyn inhibition rescues established memory and synapse loss in Alzheimer mice. Ann.Neurol. 2015 PMID: 25707991
• Green Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol.Oncol. 2009 PMID: 19393585
• De Wispelaere The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via Fyn kinase. J.Virol. 2013 PMID: 23616652
• Hennequin 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. 2006 PMID: 17064066