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VEGFR-3-IN-1

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Catalog No. T72924Cas No. 2756668-73-0

VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. It exhibits antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells.

VEGFR-3-IN-1

VEGFR-3-IN-1

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Purity: 99.95%
Catalog No. T72924Cas No. 2756668-73-0
VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. It exhibits antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$48In StockIn Stock
5 mg$113In StockIn Stock
10 mg$189In StockIn Stock
25 mg$378In StockIn Stock
50 mg$619In StockIn Stock
100 mg$993-In Stock
500 mg$1,980-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Batch Information

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Purity:99.95%
Appearance:Solid
Color:White
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COA LCMS HNMR

Product Introduction

VEGFR-3-IN-1 AI Summary
VEGFR-3-IN-1 exhibits a range of bioactivities including potent anticancer activity against human MDA-MB-231 and MDA-MB-436 cells with IC50 values of 2220.0 nM and 3500.0 nM, respectively. It inhibits VEGFR3, FLT4, MELK, BTK, KDR/VEGFR2, and FLT1/VEGFR1 with varying levels of activity and IC50 values. The compound also displays antiproliferative activity against VEGF-C- and VEGF-D-induced human dermal lymphatic endothelial cells with IC50 values of 250.0 nM and 680.0 nM, respectively, and induces apoptosis in MDA-MB-231 and MDA-MB-436 cells. In vivo studies in Sprague-Dawley rats show favorable pharmacokinetic properties, including half-life, Cmax, AUC, volume of distribution, clearance, and bioavailability. Additionally, it demonstrates significant antitumor activity against MDA-MB-231 cell xenografts in BALB/c mice, leading to tumor growth inhibition, with a maximum tolerated dose (MTD) of 300.0 mg/kg in po dosed BALB/c mice..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. It exhibits antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells.
Targets&IC50
VEGFR3:110.4 nM
In vitro
VEGFR-3-IN-1 (50, 25 mg/kg; oral; once; nude mice) achieved the most potent tumor volume inhibition in nude mice, with an inhibition rate of 61.9%.The results of VEGFR-3-IN-1 (10 mg/kg; oral) post-treatment showed a maximal concentration (Cmax) of 420 ng/mL, an AUC0-t of 9219 ng-h /mL, AUC0-∞ of 12,304 ng-h/mL, and a half-life (t1/2) of 16 hours.
In vivo
VEGFR-3-IN-1 (50, 25 mg/kg; oral; once; nude mice) achieved the most potent tumor volume inhibition in nude mice, with an inhibition rate of 61.9%.The results of VEGFR-3-IN-1 (10 mg/kg; oral) post-treatment showed a maximal concentration (Cmax) of 420 ng/mL, an AUC0-t of 9219 ng-h /mL, AUC0-∞ of 12,304 ng-h/mL, and a half-life (t1/2) of 16 hours.
Chemical Properties
Molecular Weight616.1
FormulaC29H29ClF3N7OS
Cas No.2756668-73-0
SmilesC(NC1=CC(C(F)(F)F)=C(Cl)C=C1)(=O)N2CCN(C3=C4C(SC(=C4)C5=CC=C(C=C5)N6CCN(C)CC6)=NC=N3)CC2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 1 mg/mL (1.62 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.62 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6231 mL8.1156 mL16.2311 mL81.1557 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

VEGFR3
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