AZM475271 (M475271) is an orally active, potent and selective inhibitor against src family kinases src and yes (IC50 = 25 nM & 10 nM, respectively; lck/VEGFR2/EGFR/csk/FGFR1 IC50 = 0.2/0.5/0.6/7.6/∼20 μM) that effectively suppresses src-dependent cellular signaling events (26%/48% inhibition of 50 ng/mL VEGF-induced HUVEC proliferation/migration at 100 nM; 31%/72% inhibition of 10 ng/mL VEGF-induced Flk-1/Src phosphorylation in HUVECs at 300 nM) and exbihits anticancer efficacy both in cultures (70% PC-9/30% A549 proliferation inhibition at 1 μM) and in vivo (78%/100% PC-9 tumor growth suppression in mice via 10/50 mg/kg/day p.o.).
Orally active, potent and selective src and yes inhibitor with anticancer efficacy both in cultures and in mice in vivo.
Journal of pharmacological sciences, 98(2), 130-141 (2005-06-07)
Vascular endothelial growth factor (VEGF) was reported to be a potent proangiogenic factor that plays a pivotal role in both physiological and pathological angiogenesis. M475271, 4-quinazolinamine, N-(2-chloro-5-methoxyphenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl) methoxy]-(9Cl), is a new anilinoquinazoline derivative that showed selective inhibition of Src kinase
Triple-negative breast cancer (TNBC) has a high risk of relapse and there are few chemotherapy options. Although 5-hydroxytryptamine (5-HT, serotonin) signaling pathways have been suggested as potential targets for anti-cancer drug development, the mechanism responsible for the action of 5-HT
Anti-cancer agents in medicinal chemistry, 17(7), 966-972 (2016-09-28)
Earlier results from our group have shown that in pancreatic ductal adenocarcinoma (PDAC)-derived cells transforming growth factor (TGF)-β1-dependent epithelial-mesenchymal transition (EMT) and cell motility was inhibited by the Src inhibitors PP2 and PP1 both of which targeted the TGF-β receptors
Src, a proto-oncogene, has been strongly implicated in the growth, progression and metastasis of a number of human cancers. Its role in lung cancer is, however, still unknown. In the present study, we assessed the expression of Src in three
5-Hydroxytryptamine (5-HT) induces proliferation of cancer cells and vascular cells. In addition to 5-HT production by several cancer cells including gastrointestinal and breast cancer, a significant level of 5-HT is released from activated platelets in the thrombotic environment of tumors
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