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EG00229

CAS No. : 1210945-69-9

MCE 站：EG00229

产品活性：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。

研究领域：Immunology/Inflammation

作用靶点：Complement System

In Vitro: 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.

In Vivo: EG00229 (0-10 mg/kg; intraperitoneal injection; three times per week; for 4 weeks; NSG mice) treatment substantially reduces tumor growth and visible vascularization.

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