VEGFR-3-IN-1 |
| Catalog No.GC64205 |
VEGFR-3-IN-1 es un inhibidor de VEGFR3 potente y selectivo con una IC50 de 110,4 nM. VEGFR-3-IN-1 inhibe significativamente la proliferaciÓn y migraciÓn de células endoteliales linfÁticas dérmicas humanas (HDLEC) inducidas por VEGF-C, células MDA-MB-231 y MDA-MB-436 al inactivar la vÍa de seÑalizaciÓn de VEGFR3, y también de manera efectiva inhibe el crecimiento del cÁncer de mama.
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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *