|
产品描述： Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM. |
|
靶点：
IC50: 92-112 nM (BRD2, BRD3, BRD4);EpigeneticReaderDomain |
体内研究：
In MDA-MB-231 murine xenografts, tumor mass is significantly (p < 0.05) reduced by Birabresib (OTX-015) (50 mg/kg) with respect to vehicle-treated animals. Birabresib (OTX-015) in combination with 2 mg/kg RAD001 shows more effective activity than Birabresib alone |
参考文献：
1. J. Kay Noel, et al. Abstract C244: Development of the BET bromodomain inhibitor OTX015. Mol Cancer Ther November 2013 12; C244. 2. Marie-Magdelaine Coudé, et al. BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget. 2015 Jul 10; 6(19): 17698–17712. 3. Lu P, et al. The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb. Sci Rep. 2016 Apr 12;6:24100 4. Vázquez R, et al. The bromodomain inhibitor OTX015 (MK-8628) exerts anti-tumor activity in triple-negative breast cancer models as single agent and in combination with RAD001. Oncotarget. 2017 Jan 31;8(5):7598-7613. |
|
溶解性：
DMSO : ≥ 49 mg/mL (99.60 mM) |
|
保存条件：
-20℃ |
配置溶液浓度参考：
|
1mg |
5mg |
10mg |
| 1 mM |
2.033 ml |
10.163 ml |
20.326 ml |
| 5 mM |
0.407 ml |
2.033 ml |
4.065 ml |
| 10 mM |
0.203 ml |
1.016 ml |
2.033 ml |
| 50 mM |
0.041 ml |
0.203 ml |
0.407 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京