Saracatinib | Src family kinase inhibitor

Saracatinib (379231-04-6) is a potent and selective inhibitor of Src family kinases, IC₅₀=4-10 nM for Src, c-Yes, Fyn, Lyn, Blk, Fgr and Lck.¹ Demonstrates potent antimigratory, anti-invasive and antiproliferative activity and inhibits metastasis in a mouse model of bladder cancer.² Inhibits MERS- CoV at early stages of the viral life cycle at mM concentrations.^3,4  Rescues memory performance and reduces phospho-Tau accumulation in traumatic tauopathy.⁵ Rescues memory deficits and synaptic depletion in an Alzheimer’s mouse model.⁶

References:

1. 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
2. Green et al. (2009), Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530; Oncol., 3 248
3. de Wispelaere et al. (2013), The small molecules AZD0530 and Dasatinib inhibit dengue virus RNA replication via Fyn kinase; Virol., 87 7367
4. Shin et al. (2018), Saracatinib Inhibits Middle East Respiratory Syndrome-Coronavirus Replication In Vitro; Viruses, 10 283
5. Tang et al. (2020), Fyn kinase inhibition reduces protein aggregation, increases synapse density and improves memory in transgenic mice and traumatic Tauopathy; Acta Neuropathol. Commun., 8 96
6. Kaufman et al. (2015), Fyn inhibition rescues established memory and synapse loss in Alzheimer mice; Neurol., 77 953