Shopping Cart
- Remove All
- Your shopping cart is currently empty
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 | Availability | Quantity |
---|---|---|---|
1 mg | $130 | In Stock | |
5 mg | $290 | In Stock | |
10 mg | $480 | In Stock | |
25 mg | $950 | 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 | 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 | 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 |
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 | ||||||||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.