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AD4

Name: AD4
Brand: TargetMol
SKU: T78805
Rating: 4.5 (1 reviews)

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Catalog No. T78805Cas No. 2918262-09-4

AD4 is an artemisinin-derived proteolysis targeting chimera that selectively degrades PCLAF protein with subnanomolar potency in RS4;11 leukemia cells,AD4 leads to activation of the p21/Rb signaling axis, robust anti-tumor activity, and significantly prolonged survival in RS4;11 xenograft NOD/SCID mouse models, demonstrating both in vitro and in vivo therapeutic efficacy.

AD4

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Catalog No. T78805Cas No. 2918262-09-4

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	Inquiry	Inquiry	Inquiry
50 mg	Inquiry	Inquiry	Inquiry

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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	AD4 is an artemisinin-derived proteolysis targeting chimera that selectively degrades PCLAF protein with subnanomolar potency in RS4;11 leukemia cells,AD4 leads to activation of the p21/Rb signaling axis, robust anti-tumor activity, and significantly prolonged survival in RS4;11 xenograft NOD/SCID mouse models, demonstrating both in vitro and in vivo therapeutic efficacy.
Targets&IC50	PCLAF:0.6 nM
In vitro	AD4 functions as a bifunctional PROTAC that recruits an E3 ubiquitin ligase to the PCLAF protein. Mechanistically, it utilizes an Artemisinin-based scaffold as a warhead to bind PCLAF, facilitating its proximity to the E3 ligase. This interaction leads to the polyubiquitination of PCLAF and its subsequent degradation via the proteasome pathway. In cellular assays, AD4 exhibits an IC50 of 0.6 nM against PCLAF. The depletion of PCLAF levels results in the disruption of DNA repair mechanisms and the suppression of tumor cell proliferation [1].

Chemical Properties

Molecular Weight	1035.23
Formula	C₅₅H₇₈N₄O₁₅
Cas No.	2918262-09-4
Smiles	C[C@@H]1[C@]2([C@]34[C@@](O[C@](C)(OO3)CC[C@]4([C@H](C)CC2)[H])(O[C@@H]1OCCN(CCO[C@H]5O[C@]6([C@]78[C@]([C@H]5C)(CC[C@@H](C)[C@@]7(CC[C@](C)(O6)OO8)[H])[H])[H])C(CCCCCCCNC9=C%10C(C(=O)N(C%10=O)C%11C(=O)NC(=O)CC%11)=CC=C9)=O)[H])[H]

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: 80 mg/mL (77.28 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.9660 mL	4.8298 mL	9.6597 mL	48.2984 mL
5 mM	0.1932 mL	0.9660 mL	1.9319 mL	9.6597 mL
10 mM	0.0966 mL	0.4830 mL	0.9660 mL	4.8298 mL
20 mM	0.0483 mL	0.2415 mL	0.4830 mL	2.4149 mL
50 mM	0.0193 mL	0.0966 mL	0.1932 mL	0.9660 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

AD4

AD4

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