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FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $74 | In Stock | In Stock | |
| 5 mg | $163 | In Stock | In Stock | |
| 10 mg | $239 | In Stock | In Stock | |
| 25 mg | $393 | In Stock | In Stock | |
| 50 mg | $598 | In Stock | In Stock |
| Description | FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V. |
| In vitro | FKBP12 PROTAC dTAG-13 selectively degrades FKBP12^F36V fusion proteins without affecting wild-type FKBP12. In 293T, PATU-8988T, and EOL-1 cells, FKBP12 PROTAC dTAG-13 (500 nM, 4 h) effectively degraded FKBP12^F36V-KRAS^G12V or FKBP12^F36V-ABL1 and suppressed downstream signaling. Dose-dependent degradation was observed from 10 to 500 nM[1]. |
| In vivo | In NOD/SCID mice bearing PATU-8988T FKBP12^F36V-KRAS^G12V xenografts, a single intraperitoneal dose of FKBP12 PROTAC dTAG-13 (35 mg/kg) reduced fusion protein levels in tumors within 2 h, lasting ≥12 h[1]. |
| Synonyms | dTAG-13 |
| Molecular Weight | 1049.17 |
| Formula | C57H68N4O15 |
| Cas No. | 2064175-41-1 |
| Smiles | O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCCCCCCNC(COC4=C([C@H](OC(=O)[C@H]5N(C([C@@H](CC)C6=CC(OC)=C(OC)C(OC)=C6)=O)CCCC5)CCC7=CC(OC)=C(OC)C=C7)C=CC=C4)=O |
| Relative Density. | 1.260 g/cm3 (Predicted) |
| Storage | store at low temperature | 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 (76.25 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (3.15 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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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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