VEGFR-3-IN-1

Research use only, not for human use.

VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM.

VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 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.

VEGFR-3-IN-1 (compound 38k) exhibits a significantly higher antiproliferative activity on MDA-MB-231 and MDA-MB-436 cells than 10 (IC50 > 50 μM), with IC50 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.Cell Viability Assay Cell 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 Analysis Cell Line:HDLEC cells Concentration:10-500 nM Incubation Time:Result: Antilymphangiogenic activities of VEGFR-3-IN-1 by suppressing the expression of VEGFR3.

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 Cmax, AUC0-t , AUC0-∞ and t1/2 values of 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively.Animal Model:Nude mice (carrying xenografted BC)Dosage:50 mg/kgAdministration: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 Cmax, AUC0-t , AUC0-∞ and t1/2 were 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively.

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Angiogenesis

VEGFR

VEGFR

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2756668-73-0

616.1

C29H29ClF3N7OS

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (20.29 mM; ultrasonic and warming and adjust pH to 6 with HCl and heat to 60°C )

C(NC1=CC(C(F)(F)F)=C(Cl)C=C1)(=O)N2CCN(C3=C4C(SC(=C4)C5=CC=C(C=C5)N6CCN(C)CC6)=NC=N3)CC2

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(-20℃)

With Ice Pack

≥ 2 years