EG00229,98.18%

产品编号:Bellancom-10799| CAS NO:1210945-69-9| 分子式:C19H20F3N7O7S3| 分子量:611.60

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-10799
1400.00 杭州 北京(现货)
Bellancom-10799
2250.00 杭州 北京(现货)
Bellancom-10799
8980.00 杭州 北京(现货)
Bellancom-10799
15400.00 杭州 北京(现货)

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EG00229

产品介绍 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。
生物活性

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
性状Solid
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 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 西域 网站选购。
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)

参考文献

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