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dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12F36V fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12F36V-Nluc in vivo.

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dTAGV-1 TFA Chemical Structure

dTAGV-1 TFA Chemical Structure

CAS No. : 2624313-15-9

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Based on 1 publication(s) in Google Scholar

Other Forms of dTAGV-1 TFA:

dTAGV-1 TFA Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

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Description

dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12F36V fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12F36V-Nluc in vivo[1].

IC50 & Target[1]

VHL

 

In Vitro

dTAGV-1 (0.1 nM-10 μM; 24 h) TFA induces potent degradation of FKBP12F36V-Nluc with no effects on FKBP12WT-Nluc in 293FT cells[1].
dTAGV-1 (125-2000 nM; 24 h) TFA co-treatment with THAL-SNS-032 leads to pronounced degradation of both LACZ-FKBP12F36V and CDK9[1].
dTAGV-1 (500 nM; 1-24 h) TFA leads to rapid KRASG12V and pERK1/2 degradation[1].
dTAGV-1 (50-5000 nM; 24 h) TFA enables EWS/FLI degradation in Ewing sarcoma[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

dTAGV-1 TFA Related Antibodies
In Vivo

dTAGV-1 (35 mg/kg; i.p. once daily for 4 days) TFA induces degradation of FKBP12F36V-Nluc in mice[1].
dTAGV-1 (2-10 mg/kg; i.p.) TFA exhbits half-lives (T1/2=3.64 and 4.4 h), Cmax (595 and 2123 ng/mL) and great exposure (AUCinf?=3136 and?18517 h?ng/mL) in mice[1].
dTAGV-1 (2 mg/kg; i.v.) TFA exhbits half-life (T1/2=3.02 h), Cmax (7780 ng/mL) and great exposure (AUCinf?=3329 h?ng/mL) in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12F36V cells[1]
Dosage: 35 mg/kg
Administration: I.p. once daily for 4 days
Result: Observed striking loss of bioluminescent signal 4 h after the first and three administrations.
Degradation evident 28 h after the final administration.
Molecular Weight

1361.56

Formula

C70H91F3N6O16S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C(F)(F)F)=O.O=C([C@H]1N(CCCC1)C([C@H](C2=CC(OC)=C(C(OC)=C2)OC)CC)=O)O[C@@H](C3=C(C=CC=C3)OCC(NCCCCCCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)=O)=O)=O)CCC7=CC(OC)=C(C=C7)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 37.5 mg/mL (27.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.7345 mL 3.6723 mL 7.3445 mL
5 mM 0.1469 mL 0.7345 mL 1.4689 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.75 mg/mL (2.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 3.75 mg/mL (2.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

SDS (393 KB)

COA (253 KB) HNMR (488 KB) RP-HPLC (248 KB) LCMS (103 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.7345 mL 3.6723 mL 7.3445 mL 18.3613 mL
5 mM 0.1469 mL 0.7345 mL 1.4689 mL 3.6723 mL
10 mM 0.0734 mL 0.3672 mL 0.7345 mL 1.8361 mL
15 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2241 mL
20 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9181 mL
25 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7345 mL
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dTAGV-1 TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

dTAGV-12624313-15-9dTAGV1dTAGV 1PROTACsFKBP12F36VdegradationInhibitorinhibitorinhibit

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