VEGFR-3-IN-1

VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC 50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth In Vitro VEGFR-3-IN-1 (compound 38k) exhibits a significantly higher antiproliferative activity on MDA-MB-231 and MDA-MB-436 cells than 10 (IC 50 > 50 μM), with IC 50 values of 2.22 and 3.50 μM, respectively. VEGFR-3-IN-1 markedly suppresses the phosphorylation of VEGFR3 and its downstream proteins in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MDA-MB-231 and MDA-MB-436 cells Concentration: 100 nM Incubation Time: 48 hours Result: Exerted antimigration and antiproliferative activities through targeting VEGFR3 in MDA-MB-231 and MDA-MB-436 cells. Western Blot AnalysisCell Line: HDLEC cells Concentration: 10-500 nM Incubation Time: Result: Antilymphangiogenic activities of VEGFR-3-IN-1 by suppressing the expression of VEGFR3. In Vivo VEGFR-3-IN-1 (50, 25 mg/kg; p.o.) reduces the tumor volume, and displays the strongest inhibitory activity in mice, with a growth inhibition rate of 61.9% . VEGFR-3-IN-1 (10 mg/kg; p.o.) treatment shows the C max , AUC 0-t , AUC 0-∞ and t 1/2 values of 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice (carrying xenografted BC) Dosage: 50 mg/kg Administration: P.o.;once Result: Reduced the tumor volume, and displayed the strongest inhibitory activity in mice. Animal Model: Sprague-Dawley (SD) rats Dosage: 10 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The C max , AUC 0-t , AUC 0-∞ and t 1/2 were 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively. Form:Solid IC50& Target:VEGFR3 110.4 nM (IC 50 )

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