EG01377 dihydrochloride

Name: EG01377 dihydrochloride
Brand: MedChemExpress
SKU: HY-112151A
Rating: 5.0 (5 reviews)

製品番号: HY-112151A 純度: 98.98%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a K_d of 1.32 μM, and IC₅₀s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 2749438-61-5

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 551	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 551	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$150	在庫あり	Estimated Time of Arrival: December 31
5 mg	$380	在庫あり	Estimated Time of Arrival: December 31
10 mg	$580	在庫あり	Estimated Time of Arrival: December 31
25 mg	$950	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1250	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1680	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of EG01377 dihydrochloride:

EG01377 在庫あり

顧客検証

Cell Proliferation/Viability Assay

: EG01377 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 25;14(2):159. [Abstract]; EG01377 (20, 40, 80 µM) attenuates the phosphorylation of EGFR, AKT, GSK3β, and mTOR in PC-3 and DU-145 cells.

: EG01377 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 25;14(2):159. [Abstract]; EG01377 (20, 40, 80 µM; 14 days) significantly attenuates clone formation ability of PC-3 and DU-145 cells in a concentration-dependent manner.

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

IC50: 609 nM (NRP1-a1 and NRP1-b)^[1]

体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC₅₀ of 30 μM.

体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 (T_1/2) of 4.29 h.

分子量

659.60

分子式

C₂₆H₃₂Cl₂N₆O₆S₂

CAS 番号

2749438-61-5

Appearance

Solid

Color

White to off-white

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 200 mg/mL (303.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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	0.7580 mL	1.5161 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 98.98%

Select Batch:

データシート (282 KB) SDS (252 KB)

COA (258 KB) RP-HPLC (266 KB) MS (177 KB)

取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5161 mL	7.5804 mL	15.1607 mL	37.9018 mL
	5 mM	0.3032 mL	1.5161 mL	3.0321 mL	7.5804 mL
	10 mM	0.1516 mL	0.7580 mL	1.5161 mL	3.7902 mL
	15 mM	0.1011 mL	0.5054 mL	1.0107 mL	2.5268 mL
	20 mM	0.0758 mL	0.3790 mL	0.7580 mL	1.8951 mL
	25 mM	0.0606 mL	0.3032 mL	0.6064 mL	1.5161 mL
	30 mM	0.0505 mL	0.2527 mL	0.5054 mL	1.2634 mL
	40 mM	0.0379 mL	0.1895 mL	0.3790 mL	0.9475 mL
	50 mM	0.0303 mL	0.1516 mL	0.3032 mL	0.7580 mL
	60 mM	0.0253 mL	0.1263 mL	0.2527 mL	0.6317 mL
	80 mM	0.0190 mL	0.0948 mL	0.1895 mL	0.4738 mL
	100 mM	0.0152 mL	0.0758 mL	0.1516 mL	0.3790 mL