Chemical Structure : DW-71177
CAS No.:
2241311-72-6
DW-71177
(DW71177, DW 71177)
Catalog No.: PC-21651Not For Human Use, Lab Use Only.
DW-71177 (DW71177) is a potent and BD1-selective BET inhibitor with ITC KD of 6.7 nM (BRD4-BD1), 20-fold selective over BRD4-BD2, exhibits strong antileukemic activity.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DW-71177 (DW71177) is a potent and BD1-selective BET inhibitor with ITC KD of 6.7 nM (BRD4-BD1), 20-fold selective over BRD4-BD2, exhibits strong antileukemic activity.
DW-71177 exhibits KD values of 5.5-13.6 nM for BD1s and 86-163 nM for BD2s in the isothermal titration calorimetry (ITC) experiments.
DW-71177 specifically targets BET bromodomains in bromodomain-selectivity profiling.
DW-71177 exhibits strong growth inhibition (GI50 <0.1 uM) for NUT midline carcinoma cell line (Ty-82), AML cell lines (MV4-11 and THP-1), and B-cell lymphoma cell lines (Pfeiffer and SU-DHL-4).
DW-71177 induces the accumulation of MV4-11 cells in the sub-G1 phase and increases the apoptotic cell population
DW-71177 (120 mg/kg) exhibits antitumor activity in an acute myeloid leukemia (AML) xenograft model.
Physicochemical Properties
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M.Wt
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384.48
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Formula
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C20H28N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-[4-(7-methoxy-1-methyl-[1,2,4]triazolo[4,3-a]quinoxalin-4-ylamino)-butyl]-3-methyl-butyramide
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References
1. Imran Ali, et al. Eur J Med Chem. 2023 Dec 16:265:116052.
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