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TDI-11055 is an orally available inhibitor of chromatin reader 11-19 leukemia (ENL) that works by blocking the interaction of its YEATS domain with acylated histones. TDI-11055 can be used to study acute myeloid leukemia (AML).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $100 | - | In Stock | |
| 5 mg | $247 | - | In Stock | |
| 10 mg | $396 | - | In Stock | |
| 25 mg | $795 | - | In Stock | |
| 50 mg | $1,220 | - | In Stock |
| Description | TDI-11055 is an orally available inhibitor of chromatin reader 11-19 leukemia (ENL) that works by blocking the interaction of its YEATS domain with acylated histones. TDI-11055 can be used to study acute myeloid leukemia (AML). |
| Targets&IC50 | AF9 YEATS domain:0.07 μmol/L, ENL YEATS domain:0.05 μmol/L |
| In vitro | Time-resolved fluorescence energy transfer (TR-FRET) assays were used to measure the inhibitory effects of TDI-11055 on the interactions between different YEATS domains and acylated histone peptides. TDI-11055 retained potency and selectivity for the YEATS domains of ENL (IC50 = 0.05 μmol/L) and AF9 (IC50 = 0.07 μmol/L) but showed no inhibition of the YEATS domains of GAS41 and YEATS2. [2] |
| In vivo | Mouse xenograft model using MV4;11 cells subcutaneously implanted into BALB/c nude mice. After tumors reached approximately 300 to 400 mm3, treatment with TDI-11055 [100 or 200 mg/kg, per os (p.o.), b.i.d.] or vehicle was initiated and continued for 8 consecutive days. Dosing with TDI-11055 twice daily resulted in significant inhibition of tumor growth over 8 days of treatment with no overt effect on body weight. Gene expression analysis of tumors at the end of treatment revealed a substantial reduction in the expression of key ENL target genes (HOXA9, MYC, MEIS1, and MYB) in tumors in the TDI-11055–-treated group compared with vehicle controls. [2] |
| Synonyms | TDI11055, TDI 11055 |
| Molecular Weight | 388.47 |
| Formula | C22H24N6O |
| Smiles | C[C@@H](CCC1)N1CC2=CC3=C(N2)C=C(NC(C4=CC(C=NN5C)=C5C=C4)=O)N=C3 |
| Color | Yellow |
| Appearance | Solid |
| 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 (205.94 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (8.49 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. | |||||||||||||||||||||||||||||||||||
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DMSO
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