DW-71177 | BET BD1 inhibitor | Probechem Biochemicals

Chemical Structure : DW-71177

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DW-71177 (DW71177, DW 71177)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	384.48
分子式	C20H28N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[4-(7-methoxy-1-methyl-[1,2,4]triazolo[4,3-a]quinoxalin-4-ylamino)-butyl]-3-methyl-butyramide

参考文献

1. Imran Ali, et al. Eur J Med Chem. 2023 Dec 16:265:116052.

DW-71177 (DW71177, DW 71177)

生物&药学活性

物理化学性质&存储条件

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DW-71177 (DW71177, DW 71177)

生物&药学活性

物理化学性质&存储条件

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