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dTAGV-1 TFA

Catalog No. T40251 Copy Product Info
Purity: 99.73%
🥰Excellent
dTAGV-1 TFA is a highly efficient, highly selective VHL-dependent PROTAC-mediated protein degrader that specifically targets and degrades mutant FKBP12 fusion proteins. dTAGV-1 TFA efficiently induces the degradation of FKBP12 fusion proteins at both the cellular and in vivo levels.

dTAGV-1 TFA

Copy Product Info
🥰Excellent
Catalog No. T40251

dTAGV-1 TFA is a highly efficient, highly selective VHL-dependent PROTAC-mediated protein degrader that specifically targets and degrades mutant FKBP12 fusion proteins. dTAGV-1 TFA efficiently induces the degradation of FKBP12 fusion proteins at both the cellular and in vivo levels.

dTAGV-1 TFA
Cas No. 2624313-15-9
Pack SizePriceUSA StockGlobal StockQuantity
1 mg$147-In Stock
5 mg$372-In Stock
10 mg$633-In Stock
25 mg$863-In Stock
50 mg$1,160-In Stock
100 mg$1,570-In Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:99.73%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
dTAGV-1 TFA is a highly efficient, highly selective VHL-dependent PROTAC-mediated protein degrader that specifically targets and degrades mutant FKBP12 fusion proteins. dTAGV-1 TFA efficiently induces the degradation of FKBP12 fusion proteins at both the cellular and in vivo levels.
In vitro
Methods: PATU-8902 FKBP12F³⁶V-KRASG¹²V cells were treated with dTAGV-1 TFA (500 nM) for 4 hours, and KRASG¹²V expression levels were detected by Western blot.
Results: dTAGV-1 TFA induced KRASG¹²V degradation (4 hours). [1]
Method: 293T WT and 293T VHL⁻/⁻ cells (both expressing FKBP12F³⁶V-KRASG¹²V) were treated with dTAGV-1 TFA (500 nM) for 4 hours, and KRASG¹²V expression levels were detected by Western blot.
Results: dTAGV-1 TFA failed to degrade KRASG¹²V in VHL⁻/⁻ cells, demonstrating that its action is VHL-dependent.[1]
In vivo
Methods: To investigate the in vivo pharmacokinetics (PK) of dTAGV-1 TFA, female NSG mice (8 weeks old) were selected. After tail vein inoculation with MV4;11 luc-FKBP12F³⁶V cells, the mice received daily intraperitoneal injections of dTAGV-1 TFA (35 mg/kg) for 3 consecutive days, followed by in vivo imaging 4 hours after the final dose.
Results: Four hours after the first administration, the bioluminescence signal in the dTAGV-1 group decreased significantly, and the degradation effect persisted 28 hours after the final administration.[1]
Chemical Properties
Molecular Weight1361.58
FormulaC70H91F3N6O16S
Cas No.2624313-15-9
SmilesC(C(O)=O)(F)(F)F.[C@@H](OC(=O)[C@H]1N(C([C@@H](CC)C2=CC(OC)=C(OC)C(OC)=C2)=O)CCCC1)(CCC3=CC(OC)=C(OC)C=C3)C4=C(OCC(NCCCCCCC(N[C@H](C(=O)N5[C@H](C(N[C@@H](C)C6=CC=C(C=C6)C=7SC=NC7C)=O)C[C@@H](O)C5)[C@](C)(C)C)=O)=O)C=CC=C4
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -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 (58.76 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.7344 mL3.6722 mL7.3444 mL36.7220 mL
5 mM0.1469 mL0.7344 mL1.4689 mL7.3444 mL
10 mM0.0734 mL0.3672 mL0.7344 mL3.6722 mL
20 mM0.0367 mL0.1836 mL0.3672 mL1.8361 mL
50 mM0.0147 mL0.0734 mL0.1469 mL0.7344 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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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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