EG01377
目录号 : GC33272
EG01377是一种神经纤毛蛋白1(neuropilin-1)拮抗剂，对NRP1-b1的Kd值为1.32μM，对NRP1-a1和NRP1-b1的IC50值均为609nM，对NRP2没有作用；EG01377具有抗血管生成，抗迁移及抗肿瘤等活性。
Cas No.:2227996-00-9
Sample solution is provided at 25 µL, 10mM.
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EG01377 is a neuropilin-1 (NRP1) antagonist, with a Kd of 1.32 μM for NRP1-b1, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1, but shows no effect on NRP2; EG01377 has antiangiogenic, antimigratory, and antitumor effects.
EG01377 is a neuropilin-1 (NRP1) antagonist, with a Kd of 1.32 μM for NRP1-b1, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1, but shows no effect on NRP2. EG01377 inhibits NRP1 in DU145/cells.Ad.NRP1 cells (IC50, 1.6 μM). EG01377 (3, 10, and 30 μM) inhibits VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR. EG01377 (30 μM) also significantly reduces HUVEC cell migration in response to VEGFA, and reduces VEGF-induced angiogenesis. Moreover, EG01377 (30 μM) in combination with VEGFA causes reduction in A375P spheroid outgrowth. EG01377 blocks the production of TGFβ by Nrp1+ Tregs in the presence of tumor cell-derived factors[1].
[1]. Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018 May 10;61(9):4135-4154.
Kinase experiment: | The 96-well plates are precoated with NP1 protein at 3 μg/mL overnight at 4°C. On the following day, the plates are treated with blocking buffer (PBS containing 1% BSA) and washed three times with wash buffer (PBS containing 0.1% Tween-20). The various concentrations of compounds (EG01377, etc.) diluted in PBS containing 1% DMSO are added, followed by addition of 0.25 nM of bt-VEGF-A165. After 2 h of incubation at room temperature, the plates are washed three times with wash buffer. The bound bt-VEGF-A165 to NP-1 is detected by streptavidin-horseradish peroxidase conjugates and the enzyme substrate, and measured using a plate reader at A450 nm with a reference wavelength at A595 nm. Nonspecific binding is determined in the absence of NP-1 coated wells of the plates[1]. |
References: [1]. Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018 May 10;61(9):4135-4154. | |
| Cas No. | 2227996-00-9 | SDF | |
| Canonical SMILES | O=S(C1=CC(C2=CC=C(CN)C=C2)=CC3=C1OCC3)(NC4=C(C(N[C@@H](CCC/N=C(N)/N)C(O)=O)=O)SC=C4)=O | ||
| 分子式 | C26H30N6O6S2 | 分子量 | 586.68 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7045 mL | 8.5225 mL | 17.0451 mL |
| 5 mM | 0.3409 mL | 1.7045 mL | 3.409 mL |
| 10 mM | 0.1705 mL | 0.8523 mL | 1.7045 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet