EG01377 dihydrochloride
目录号 : GC60149EG01377dihydrochloride是有效的、可生物利用的和选择性的neuropilin-1(NRP1)抑制剂,Kd值为1.32μM,对NRP1-a1和NRP1-b1的IC50值均为609nM。EG01377dihydrochloride具有抗血管生成,抗迁移及抗肿瘤等活性。
Sample solution is provided at 25 µL, 10mM.
EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects[1].
EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR[1].EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA[1].EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure[1].EG01377 (30 μM) reduces network area, length, and branching points[1].EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis[1].EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth[1].EG01377 (500 nM; 2 hours) blocks the production of transforming growth factor beta (TGFβ) by Nrp1+ regulatory T-cell SMAD3/AKT (Tregs) in the presence of tumor cell-derived factors[1]. Western Blot Analysis[1] Cell Line: Human umbilical vein endothelial cells (HUVECs)
EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice[1]. Animal Model: 6-8 week-old BABL/c female mice[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.
Cas No. | 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.Cl.Cl | ||
分子式 | C26H32Cl2N6O6S2 | 分子量 | 659.6 |
溶解度 | DMSO: 200 mg/mL (303.21 mM) | 储存条件 | -20°C, stored under nitrogen |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.5161 mL | 7.5804 mL | 15.1607 mL |
5 mM | 0.3032 mL | 1.5161 mL | 3.0321 mL |
10 mM | 0.1516 mL | 0.758 mL | 1.5161 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet