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AZD 5153
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZD 5153图片
CAS NO:1869912-39-9
规格:98%
分子量:479.6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4.
CAS:1869912-39-9
分子式:C25H33N7O3
分子量:479.6
纯度:98%
存储:Store at -20°C

Background:

Target: BRD4


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 [1].


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) [1].


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 [1].


Clinical trial: no data available.


Reference:
[1] 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.