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CAS No. : 379231-04-6
MCE 国际站:Saracatinib
产品活性:Saracatinib (AZD0530) 是一种有效的 Src 抑制剂,抑制 c-Src,Lck,c-YES,Lyn,Fyn,Fgr 和 Blk 的 IC50 值为 2.7-11 nM,对其他酪氨酸激酶具有选择性。
研究领域:Protein Tyrosine Kinase/RTK | Autophagy
作用靶点:Src | Autophagy
In Vitro: Saracatinib (AZD0530), an orally available Src inhibitor, demonstrates potent antimigratory and anti-invasive effects in vitro, and inhibits metastasis in a murine model of bladder cancer. Antiproliferative activity of Saracatinib varies between cell lines (IC50 of 0.2-10 μM). Saracatinib potently inhibits the proliferation of Src3T3 mouse fibroblasts and demonstrates variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib (tumor types: colon, prostate, lung, and leukemia) is observed with IC50 values of 0.2-0.7 μM. In 3-day MTS cell proliferation assays, Saracatinib inhibits proliferation of the Bcr-Abl-driven human leukemia cell line K562 with an IC50 of 0.22 μM. In the microdroplet migration assay, Saracatinib reduces the migration of human lung cancer A549 cells in a concentration-dependent manner (IC50 0.14 μM).
In Vivo: Saracatinib (AZD0530) treatment potently inhibits the proliferation of subcutaneously transplanted Src3T3 fibroblasts in mice and rats in a dose-dependent manner. In both models, significant inhibition of tumor growth is seen at doses ≥6 mg/kg/day (60% inhibition in mice and 98% inhibition in rats versus animals treated with vehicle) and, at the maximum doses investigated, complete tumor growth inhibition is observed (100% inhibition at 25 mg/kg/day in mice and 10 mg/kg/day in rats).
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