| 产品描述: | EG00229 is a neuropilin 1 (NRP1) receptor antagonist. 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 |
| 靶点: |
IC50: 8 μM (125I-VEGF-A binding to PAE/NRP1); 3 μM (bt-VEGF-A binding to purified NRP1 b1 domain) |
| 体外研究: |
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. |
| 体内研究: |
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. |
| 参考文献: |
1. Jarvis A, et al. Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. J Med Chem. 2010 Mar 11;53(5):2215-26. 2. Grun D, et al. VEGF-A acts via neuropilin-1 to enhance epidermal cancer stem cell survival and formation of aggressive and highly vascularized tumors. Oncogene. 2016 Aug 18;35(33):4379-87. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.635 ml |
8.175 ml |
16.351 ml |
| 5 mM |
0.327 ml |
1.635 ml |
3.27 ml |
| 10 mM |
0.164 ml |
0.818 ml |
1.635 ml |
| 50 mM |
0.033 ml |
0.164 ml |
0.327 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |