VEGFR-3-IN-1 - ≥98% , CAS No.2756668-73-0

CAS: 2756668-73-0 Cat. No.: V647594 Peso molecular: 616.10

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

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 )

Specifications

Especificaciones y pureza

≥98%

Mecanismos bioquímicos y fisiológicos

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 inac

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Pureza

≥98%

Nombres e identificadores

• Sonrisas canónicas: O=C(N1CCN(C2=C(C=C(C3=CC=C(N4CCN(C)CC4)C=C3)S5)C5=NC=N2)CC1)NC6=CC=C(Cl)C(C(F)(F)F)=C6
• Peso molecular: 616.10

Propiedades químicas y físicas

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