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TAK-593 is a highly potent inhibitor of VEGFR2 with IC50 value of 0.95nM [1].

TAK-593 is an imidazo [1, 2-b] pyridazine derivative. It is found to inhibit VEGFR2 with a highly potent effect in the non-RI assay using the AlphaScreen system. And in the cell proliferation assay, TAK-593 suppresses VEGF-stimulated cell growth of HUVEC with IC50 value of 0.3nM. TAK-593 is a slow-binding inhibitor and it has a long residence time on VEGFR2. Besides that, TAK-593 also has efficacy on other receptor kinases. It gives the IC50 values of 3.2nM, 1.1nM, 4.3nM and 13nM for VEGFR1, VEGFR3, PDGFRα and PDGFRβ, respectively. Moreover, TAK-593 shows significant anti-tumor efficacy in the mouse xenograft model using A549 human lung adenocarcinoma epithelial cells. Oral administration of TAK-593 twice daily at doses of 0.25mg/kg for two weeks potently inhibits tumor growth with T/C value of 34% [1].

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