EG01377 dihydrochloride 是有效的、可生物利用的和选择性的neuropilin-1 (NRP1)抑制剂,Kd值为 1.32 μM,对NRP1-a1和NRP1-b1的IC50值均为 609 nM。EG01377 dihydrochloride 具有抗血管生成,抗迁移及抗肿瘤等活性。
生物活性 | EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor ofneuropilin-1 (NRP1), with aKdof 1.32 μM, andIC50s of 609 nM for bothNRP1-a1andNRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects[1]. |
IC50& Target | IC50: 609 nM (NRP1-a1 and NRP1-b)[1] |
体外研究 (In Vitro) | 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) | Concentration: | 3, 10, 30 μM | Incubation Time: | 30 minutes | Result: | Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50of 30 μM. |
|
体内研究 (In Vivo) | 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] | Dosage: | 2 mg/kg (Pharmacokinetic Analysis) | Administration: | I.v. administration | Result: | The half time (T1/2) of 4.29 h. |
|
分子量 | |
性状 | |
Formula | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, stored under nitrogen, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture) |
溶解性数据 | In Vitro: DMSO : 200 mg/mL(303.21 mM;Need ultrasonic) 配制储备液 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 | 0.7580 mL | 1.5161 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 (stored under nitrogen, 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: ≥ 5 mg/mL (7.58 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (7.58 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 50.0 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% (20%SBE-β-CDin saline) Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (7.58 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (7.58 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 50.0 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。
|