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NRP1b1 域的结合,IC50为 3μM,但对 VEGFA 与 VEGFR-1 和 VEGFR-2 的结合没有影响。
生物活性 | EG00229 is aneuropilin 1 (NRP1) receptorantagonist. EG00229 selectively inhibitsVEGF-Abinding toNRP1b1 domain with anIC50of 3 μM, but has no effect on VEGFA binding toVEGFR-1and VEGFR-2[1]. |
IC50& Target | IC50: 8 μM (125I-VEGF-A binding to PAE/NRP1); 3 μM (bt-VEGF-A binding to purified NRP1 b1 domain)[1]. |
体外研究 (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[1]. 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[1]. EG00229 (Compound 2) selectively inhibits radiolabeled125I-VEGF-A binding to porcine aortic endothelial (PAE)/NRP1, but not VEGFR2-expressing cells, with anIC50of 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 anIC50of 23 μM[1].
Cell Viability Assay[1] 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. |
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体内研究 (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[2].
Animal Model: | 6-week old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells[2] | 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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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 41.4 mg/mL(67.69 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.6351 mL | 8.1753 mL | 16.3506 mL | 5 mM | 0.3270 mL | 1.6351 mL | 3.2701 mL | 10 mM | 0.1635 mL | 0.8175 mL | 1.6351 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.09 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.09 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.09 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.09 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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