EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2. EG00229 is a neuropilin 1 (NRP1) receptor antagonist.

EG00229 selectively inhibits radiolabeled 125I-VEGF-A binding to porcine aortic endothelial (PAE)/NRP1, but not VEGFR2-expressing cells, with an IC50 of 8 μM. EG00229 also inhibits VEGF-A binding to lung carcinoma A549 and prostate carcinoma DU145 cells, which express NRP1, but not VEGFR1 and VEGFR2, with similar potency. Binding of VEGF-A to human umbilical vein endothelial cells (HUVECs), which express VEGFR2, VEGFR1, and NRP1, is also inhibited by EG00229 with an IC50 of 23 μM.EG00229 ( 0-100 μM; 48 hours; A549 cells) treatment causes a significant reduction in cell viability over a 48 hours incubation. EG00229 demonstrates inhibition of VEGF-A binding to NRP1 and attenuates VEGFR2 phosphorylation in endothelial cells. Inhibition of migration of endothelial cells is also observed in HUVECs.

EG00229 treatment substantially reduces tumor growth and visible vascularization.

1210945-69-9

C19H20F3N7O7S3

611.6

DMSO:41.4 mg/mL (67.69 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years