IC50: 5 nM
AZD5153 is a potent, selective, and orally available inhibitor of the bromodomain and extraterminal (BET) protein BRD4, with the IC50 value of 5 nM. AZD5153 could simultaneously ligate two bromodomains in BRD4, and exert antitumor activity in multiple xenograft tumor models .
In Vitro: A quantitative immuno-fluorescent assay in U2OS cells revealed that AZD5153 could significantly disrupt BRD4 foci, with the IC50 value of 1.7 nM. Besides, AZD5153 could inhibit the proliferation of AML, MM, and DLBCL cell lines, with the majority of cell lines having a GI50 value < 25 nM. Furthermore, 200 nM AZD5153 could significantly decrease the level of mTOR pathway associated proteins in sensitive hematologic cancer cell lines (MOLP8, MV-4-11, OCILY19) .
In Vivo: In AML, MM, and DLBCL xenografted tumor mouse models, oral administration of AZD5153 at the dose of 1, 2.5, and 5mg/kg could inhibit tumor growth in a dose dependent manner .
Clinical trial: no data available.
 Rhyasen G W, Hattersley M M, Yao Y, et al. AZD5153: a novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies[J]. Molecular Cancer Therapeutics, 2016, 15(11): 2563-2574.
|Physical Appearance||A crystalline solid|
|Storage||Store at -20°C|
|Solubility||≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide|
|Canonical SMILES||COC1=NN=C2N1N=C(N3CCC(C4=CC=C(OCCN5[[email protected]](C)C(N(C)CC5)=O)C=C4)CC3)C=C2|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|