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dFKBP-1

Name: dFKBP-1
Brand: TargetMol
SKU: T18597
Rating: 4.5 (1 reviews)

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Catalog No. T18597Cas No. 1799711-22-0

dFKBP-1 is a potent PROTAC-based FKBP12 degrader incorporating the FKBP12 ligand SLF, the Thalidomide-based cereblon ligand, and a linker[1].

dFKBP-1

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Catalog No. T18597Cas No. 1799711-22-0

dFKBP-1 is a potent PROTAC-based FKBP12 degrader incorporating the FKBP12 ligand SLF, the Thalidomide-based cereblon ligand, and a linker[1].

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
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500 mg	Inquiry	Inquiry	Inquiry

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

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Product Introduction

Bioactivity

Description

dFKBP-1 is a potent PROTAC-based FKBP12 degrader incorporating the FKBP12 ligand SLF, the Thalidomide-based cereblon ligand, and a linker[1].

In vitro

dFKBP-1 significantly reduces FKBP12 levels in MV4;11 cells, achieving over an 80% decrease at 0.1 μM and a 50% decrease at 0.01 μM. Similarly to dBET1, dFKBP-1's effect on FKBP12 destabilization can be reversed by pre-treatment with Carfilzomib, MLN4924, free SLF, or free Thalidomide. The mechanism of Cereblon (CRBN)-dependent degradation was confirmed using established isogenic 293FT cell lines, both wild-type (293FT-WT) and CRBN-deficient (293FT-CRBN?/?). dFKBP-1 treatment led to a potent and dose-dependent decrease in FKBP12 in 293FT-WT cells, with no impact observed on 293FT-CRBN?/? cells[1].

Chemical Properties

Molecular Weight	1009.11
Formula	C₅₃H₆₄N₆O₁₄
Cas No.	1799711-22-0
Smiles	O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCC(NCCCCNC(CCC(NC4=CC([C@H](OC(=O)[C@H]5N(C(C(C(CC)(C)C)=O)=O)CCCC5)CCC6=CC(OC)=C(OC)C=C6)=CC=C4)=O)=O)=O
Relative Density.	1.298 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.

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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