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AD80

Name: AD80
Brand: TargetMol
SKU: T4301
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

😃Good

Catalog No. T4301Cas No. 1384071-99-1

AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.

AD80

😃Good

Purity: 99.75%

Catalog No. T4301Cas No. 1384071-99-1

AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$39	In Stock	In Stock
5 mg	$93	In Stock	In Stock
10 mg	$148	In Stock	In Stock
25 mg	$297	In Stock	In Stock
50 mg	$488	In Stock	In Stock
100 mg	$716	In Stock	In Stock
500 mg	$1,480	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$97	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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:99.75%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.
Targets&IC50	RET (V804M):0.4 nM, RET (V804L):0.6 nM
In vitro	AD80 and AD81 effectively inhibit key signaling molecules (RET, RAF, SRC, S6K) with significantly diminished mTOR activity compared to AD57 and AD58. Specifically, AD80 stands out for its proficient inhibition of the Ras–Erk pathway, showcasing a well-balanced polypharmacological profile that targets Ret, Raf, Src, Tor, and S6K, yielding high efficacy with minimal toxicity. Furthermore, AD80 demonstrates potent anti-proliferative effects on MZ-CRC-1 and TT thyroid cancer cells in vitro, likely mediated by triggering apoptosis. Additionally, AD80 uniquely suppresses S6K1 in conjunction with inhibiting the TAM family tyrosine kinase AXL, preventing S6K1 phosphorylation and its association with mTOR. This leads to a sustained inhibition of S6K1-driven signaling and protein synthesis, underscoring its therapeutic potential.
In vivo	AD80 significantly improves survival rates, rescuing 50% of mice transplanted with PTEN-deficient leukemia cells. When administered orally, both AD80 and AD81 remarkably allow 70-90% of Drosophila ptc>dRetMEN2B model animals to reach adulthood, surpassing the effectiveness of AD57. Furthermore, AD80 demonstrates superior tumor growth inhibition and minimizes body-weight fluctuations compared to vandetanib in a mouse xenograft model.
Cell Research	MZ-CRC-1 (MEN2B) and TT (MEN2A) cells are treated with AD80 (0.2 nM to 20 μM) for 7 days and cell viability is quantitated by MTT assay.
Animal Research	Mice showing established growing tumors are separated into vehicle or drug treatment groups. A similar range of tumor sizes is selected for each experiment (vehicle vs AD57; vehicle vs AD80 vs Vandetanib). Vehicle, AD57 (20 mg/kg), AD80 (30 mg/kg), or Vandetanib (50 mg/kg) are administered by oral gavage (PO; per os or by mouth) once daily, five times a week. Tumor and body weight measurements are performed 3 times a week.

Chemical Properties

Molecular Weight	473.43
Formula	C₂₂H₁₉F₄N₇O
Cas No.	1384071-99-1
Smiles	CC(C)n1nc(-c2ccc(NC(=O)Nc3cc(ccc3F)C(F)(F)F)cc2)c2c(N)ncnc12
Relative Density.	1.49 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 60 mg/mL (126.73 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	2.1122 mL	10.5612 mL	21.1224 mL	105.6122 mL
5 mM	0.4224 mL	2.1122 mL	4.2245 mL	21.1224 mL
10 mM	0.2112 mL	1.0561 mL	2.1122 mL	10.5612 mL
20 mM	0.1056 mL	0.5281 mL	1.0561 mL	5.2806 mL
50 mM	0.0422 mL	0.2112 mL	0.4224 mL	2.1122 mL
100 mM	0.0211 mL	0.1056 mL	0.2112 mL	1.0561 mL

Calculator

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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