VEGFR-3-IN-1 |
| Katalog-Nr.GC64205 |
VEGFR-3-IN-1 ist ein potenter und selektiver VEGFR3-Inhibitor mit einem IC50 von 110,4 nM. VEGFR-3-IN-1 hemmt signifikant die Proliferation und Migration von VEGF-C-induzierten humanen dermalen lymphatischen Endothelzellen (HDLEC), MDA-MB-231- und MDA-MB-436-Zellen durch Inaktivierung des VEGFR3-Signalwegs und auch effektiv hemmt das Wachstum von Brustkrebs.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2756668-73-0
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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].
[1]. Li Y, Yang G, et al. Discovery, Synthesis, and Evaluation of Highly Selective Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) Inhibitor for the Potential Treatment of Metastatic Triple-Negative Breast Cancer. J Med Chem. 2021;64(16):12022-12048.
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