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AD57 (hydrochloride)

Name: AD57 (hydrochloride)
Brand: TargetMol
SKU: T22552
Rating: 4.5 (1 reviews)

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Catalog No. T22552Cas No. 2320261-72-9

AD57, as polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer blocks the receptor tyrosine kinase RET in Drosophila (IC50: 2 nM). AD57 effectively suppresses tyrosine kinase RET, weakens the activity of numerous other kinases, and interferes with kinases downstream of RET, including Raf, Src, and S6K, providing further efficacy in preventing signaling leading to invasion, proliferation, and metabolism-related to cancer. Tyrosine kinase RET is probably sufficient to initiate a series of transformation events including medullary thyroid carcinoma, multiple endocrine neoplasias type 2A, and 2B.

AD57 (hydrochloride)

😃Good

Catalog No. T22552Cas No. 2320261-72-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$223	35 days	35 days
5 mg	$978	35 days	35 days
10 mg	$1,720	35 days	35 days

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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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Product Introduction

Bioactivity

Description	AD57, as polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer blocks the receptor tyrosine kinase RET in Drosophila (IC50: 2 nM). AD57 effectively suppresses tyrosine kinase RET, weakens the activity of numerous other kinases, and interferes with kinases downstream of RET, including Raf, Src, and S6K, providing further efficacy in preventing signaling leading to invasion, proliferation, and metabolism-related to cancer. Tyrosine kinase RET is probably sufficient to initiate a series of transformation events including medullary thyroid carcinoma, multiple endocrine neoplasias type 2A, and 2B.
In vitro	In vitro: AD57 was demonstrated to be able to inhibit tyrosine kinase RET. But the efficacy of AD57 did not correlate solely with the blockade of RET, suggesting that the targeting of additional kinases is necessary for its biological efficacy. AD57 potently dampened the pathway-related human kinases B-Raf, mTOR, S6K, and Src [1].
In vivo	In vivo: Male nu nu mice, injected subcutaneously with MEN2A cell lines, were administered AD57 (20 mg/kg) by oral gavage (per os) once daily, five times a week. AD57 inhibited the activity of relevant target kinases at 1 μM compared with the vehicle-treated nude mice transplanted with MEN2A cells [1].

Chemical Properties

Molecular Weight	491.9
Formula	C₂₂H₂₁ClF₃N₇O
Cas No.	2320261-72-9
Smiles	Cl.CC(C)n1nc(-c2ccc(NC(=O)Nc3cccc(c3)C(F)(F)F)cc2)c2c(N)ncnc12

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

Ethanol: ≤5 mg/mL, Sonication is recommended.

DMSO: 10 mg/mL (20.33 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0329 mL	10.1647 mL	20.3293 mL	101.6467 mL
5 mM	0.4066 mL	2.0329 mL	4.0659 mL	20.3293 mL
10 mM	0.2033 mL	1.0165 mL	2.0329 mL	10.1647 mL
20 mM	0.1016 mL	0.5082 mL	1.0165 mL	5.0823 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:

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