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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.

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 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 |
| 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] |
| Molecular Weight | 1361.58 |
| Formula | C70H91F3N6O16S |
| Cas No. | 2624313-15-9 |
| Smiles | C(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 | 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 (58.76 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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. | |||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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