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Vepafestinib

Name: Vepafestinib
Brand: TargetMol
SKU: T9445
Price: 132 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9445 Copy Product Info

Purity: 98.56%

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Vepafestinib is an orally administered, highly selective, ATP-competitive RET kinase inhibitor that effectively suppresses both wild-type RET and key drug-resistant mutations (V804, G810, L730). Vepafestinib exhibits blood-brain barrier penetration and high kinase selectivity. It is suitable for use in tumor research.

Cas No. 2129515-96-2

Pack Size	Price	USA Stock	Global Stock
1 mg	$132	-	In Stock
5 mg	$328	-	In Stock
10 mg	$487	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.56%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Vepafestinib is an orally administered, highly selective, ATP-competitive RET kinase inhibitor that effectively suppresses both wild-type RET and key drug-resistant mutations (V804, G810, L730). Vepafestinib exhibits blood-brain barrier penetration and high kinase selectivity. It is suitable for use in tumor research.
In vitro	Methods: Ba/F3 cells expressing KIF5B-RET wild-type or G810 mutant were treated with different concentrations of Vepafestinib (0.1, 1, 10, 100 nM) for 2 hours, followed by detection of RET and ERK phosphorylation levels. Results: Vepafestinib exhibited potent inhibitory effects against all tested RET mutations, including solvent-front mutations G810R/S/C. [1]
In vivo	Methods: LC-2/ad lung cancer cells expressing KIF5B-RET were intracerebrally implanted into the brains of immunodeficient mice to establish a brain metastasis model. Vepafestinib was administered orally via gavage at a dose of 30 mg/kg once daily for 14 days. Results: Vepafestinib significantly prolonged survival in mice. [1]

Chemical Properties

Molecular Weight	474.55
Formula	C₂₆H₃₀N₆O₃
Cas No.	2129515-96-2
Smiles	COCc1ccc(NC(=O)c2c(C#CCN3CCOCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Relative Density.	1.33 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (94.83 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.11 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

	1mg	5mg	10mg	50mg
1 mM	2.1073 mL	10.5363 mL	21.0726 mL	105.3630 mL
5 mM	0.4215 mL	2.1073 mL	4.2145 mL	21.0726 mL
10 mM	0.2107 mL	1.0536 mL	2.1073 mL	10.5363 mL
20 mM	0.1054 mL	0.5268 mL	1.0536 mL	5.2681 mL
50 mM	0.0421 mL	0.2107 mL	0.4215 mL	2.1073 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.