1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. VEGFR-3-IN-1

VEGFR-3-IN-1 

Cat. No.: HY-132305
Handling Instructions

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.

For research use only. We do not sell to patients.

VEGFR-3-IN-1 Chemical Structure

VEGFR-3-IN-1 Chemical Structure

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Description

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[1].

IC50 & Target[1]

VEGFR3

110.4 nM (IC50)

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 (IC50 > 50 μM), with IC50 values of 2.22 and 3.50 μM, respectively[1].
VEGFR-3-IN-1 markedly suppresses the phosphorylation of VEGFR3 and its downstream proteins in a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

Cell 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%[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (carrying xenografted BC)[1]
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 [1]
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.
Molecular Weight

616.10

Formula

C₂₉H₂₉ClF₃N₇OS

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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VEGFR-3-IN-1
Cat. No.:
HY-132305
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