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Description: Potent and selective Src tyrosine kinase family inhibitor; anticancer; antiviral; orally bioavailable
Alternative Names: AZD 0530
Chemical Name: N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-4-quinazolinamine
Purity: ≥98% (HPLC)

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.

Compound Libraries for Saracatinib

Saracatinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Saracatinib

M. Wt 542.03
Formula C27H32ClN5O5
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 379231-04-6
PubChem ID 10302451

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
DMSO 10.84 20
ethanol 54.2 100

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.

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

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Product Datasheets for Saracatinib

Certificate of Analysis / Product Datasheet
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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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