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TDI-11055
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).
Catalog No. T87946
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TDI-11055
Catalog No. T87946
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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $130 | In Stock | |
| 5 mg | $290 | In Stock | |
| 10 mg | $480 | In Stock | |
| 25 mg | $950 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| 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 | ENL YEATS domain:0.05 μmol/L, AF9 YEATS domain:0.07 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] |
| Alias | TDI 11055, TDI11055 |
| Molecular Weight | 388.47 |
| Formula | C22H24N6O |
Storage & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (205.94 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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