Saracatinib

Biological Activity

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

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.

Background References

1. 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.
   Hennequin et al.
   J.Med.Chem., 2006;49:6465
2. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530.
   Green et al.
   Mol.Oncol., 2009;3:248
3. The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via Fyn kinase.
   De Wispelaere et al.
   J.Virol., 2013;87:7367
4. Fyn inhibition rescues established memory and synapse loss in Alzheimer mice.
   Kaufman et al.
   Ann.Neurol., 2015;77:953

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