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AP1867 (FK506-binding protein) is a synthetic FKBP12 F36V-directed ligand attached to 320 substituted tetrahydrooxazepines (THOXs). AP1867 (FK506-binding protein) was synthesized via combined liquid- and solid-phase methods employing sequential Mitsunobu displacements followed by ruthenium-mediated olefin metathesis to close seven-membered rings; the resin-bound THOX ligands were coupled to AP1867 in parallel, yielding candidate heterodimerizers that demonstrated membrane permeability and bioactivity in human fibrosarcoma cells, facilitating the study of targeted protein interactions and intracellular modulation.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $148 | - | In Stock | |
| 5 mg | $372 | - | In Stock | |
| 10 mg | $558 | - | In Stock | |
| 25 mg | $987 | - | In Stock | |
| 50 mg | $1,550 | - | In Stock | |
| 100 mg | $2,330 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $568 | - | In Stock |
| Description | AP1867 (FK506-binding protein) is a synthetic FKBP12 F36V-directed ligand attached to 320 substituted tetrahydrooxazepines (THOXs). AP1867 (FK506-binding protein) was synthesized via combined liquid- and solid-phase methods employing sequential Mitsunobu displacements followed by ruthenium-mediated olefin metathesis to close seven-membered rings; the resin-bound THOX ligands were coupled to AP1867 in parallel, yielding candidate heterodimerizers that demonstrated membrane permeability and bioactivity in human fibrosarcoma cells, facilitating the study of targeted protein interactions and intracellular modulation. |
| In vitro | AP1867 binds to wild-type FKBP with a Kd value of 67 nM [2]. |
| Synonyms | AP-1867, AP 1867 |
| Molecular Weight | 693.78 |
| Formula | C38H47NO11 |
| Cas No. | 195514-23-9 |
| Smiles | [C@H](C(=O)N1[C@H](C(O[C@H](CCC2=CC(OC)=C(OC)C=C2)C3=CC(OCC(O)=O)=CC=C3)=O)CCCC1)(CC)C4=CC(OC)=C(OC)C(OC)=C4 |
| Relative Density. | 1.214 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | keep away from direct sunlight,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 (115.31 mM), Sonication is recommeded. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (4.76 mM), Sonication is recommeded. 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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