Saracatinib

Name: Saracatinib
Brand: Tocris Bioscience
SKU: 7189

Tocris Bioscience a Bio-Techne Brand

Catalog # 7189

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Key Product Details

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)
Molecular Weight:	542.03

View Full Technical Details for Saracatinib

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
InChi Key	OUKYUETWWIPKQR-UHFFFAOYSA-N
Smiles	CN1CCN(CCOC2=CC3=C(C(NC4=C5OCOC5=CC=C4Cl)=NC=N3)C(OC3CCOCC3)=C2)CC1

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 for Saracatinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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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Reconstitution Calculator

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References for Saracatinib

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
De Wispelaere The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via Fyn kinase. J.Virol. 2013 PMID: 23616652
Green Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol.Oncol. 2009 PMID: 19393585
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

Citations for Saracatinib

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