EG00229

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EG00229 是一种神经纤维蛋白 1 受体 (NRP1) 拮抗剂。EG00229 选择性抑制 VEGF-A 与 NRP1 b1 域的结合， IC50 为 3μM，但对 VEGFA 与 VEGFR-1 和 VEGFR-2 的结合没有影响。

EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with anIC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2.

EG00229 (Compound 2; 0-100 μM; 48 hours; A549 cells) treatment causes a significant reduction in cell viability over a 48 hours incubation.?EG00229 (Compound 2) 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 (Compound 2) 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.Cell Viability Assay Cell Line:A549 cells Concentration:0 μM, 10 μM, 30 μM, 100 μM Incubation Time:48 hours Result:Caused a significant reduction in cell viability.

EG00229 (0-10 mg/kg; intraperitoneal injection; three times per week; for 4 weeks; NSG mice) treatment substantially reduces tumor growth and visible vascularization.Animal Model:6-week old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells Dosage:0 mg/kg, 10 mg/kg Administration:Intraperitoneal injection; three times per week; for 4 weeks Result:Reduces tumor growth and visible vascularization.

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1210945-69-9

611.6

C19H20F3N7O7S3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 41.4 mg/mL (67.69 mM )

OC(=O)C(F)(F)F.NC(=N)NCCC[C@H](NC(=O)c1sccc1NS(=O)(=O)c1cccc2nsnc12)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years