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OTX-015
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。
OTX-015图片
CAS NO:202590-98-5
规格:98%
分子量:491.99
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
BRD inhibitor
CAS:202590-98-5
分子式:C25H22ClN5O2S
分子量:491.99
纯度:98%
存储:Store at -20°C

Background:

OTX-015 is a potent inhibitor of BRD2, BRD3, and BRD4 with IC50 values range from 92 to 112 nM [1].
BRD2, BRD3, and BRD4 belong to BET bromodomain family and play an important role in regulating transcription. BRDs regulate several oncogenes transcription in a variety of cancers and thus have emerged as a promising target [2].
OTX-015 is a selective BRD2, BRD3, and BRD4 inhibitor and inhibits the binding of BRD2, BRD3, and BRD4 to AcH4. Using TR-FRET method and CHO cell lysate harboring BRD2, BRD3, and BRD4 to research the effect of OTX-015, result showed that OTX-015 inhibited BET family binding to AcH4 in a dose-dependent manner and the EC50 values range from 10 to 19 nM. When tested with human tumor cell lines, incubation with OTX-015 for 72 hours inhibited cell proliferation with GI 50 values ranged from 60 to 200 nM [1]. In ALKpos ALCL cell lines, treatment of OTX-015 for 24 h arrested cell proliferation in G1 phase which was more pronounced at 48 h and 72 h, and tested with SUPM2/TS and JB-6 cell lines OTX-015 showed ability to increase cell death rate [3].
In BLAB/c-nu/nu mice model with established Ty82 BRD-NUT midline carcinoma xenografts, oral administration of OTX-015 markedly inhibited tumor growth and reduced tumor volume [1].
参考文献:
[1]. J. Kay Noel, Kazunori Iwata, Shinsuke Ooike, et al. Development of the BET bromodomain inhibitor OTX015 [J]. Mol Cancer Ther November 2013 12; C244.
[2]. Fu LL, Tian M, Li X, et al. Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery [J]. Oncotarget. 2015 Mar 20;6(8):5501-5516.
[3]. Michela Boi, Maria Todaro, Valentina Vurchio, et al. OTX015, a bromodomain and extraterminal inhibitor, represents a novel agent for ALK positive anaplastic large cell lymphoma [J]. Mol Cancer Ther November 2013 12; A219.