| 产品描述： | STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress. |
| 靶点： |
IRE1 |
| 体外研究： |
STF-083010 shows cytostatic and cytotoxic activity in a dose- and time-dependent manner. Treatment with STF-083010 shows significant antimyeloma activity in model human multiple myeloma (MM) xenografts. RPMI 8226 human MM cells grown as tumor xenografts are treated in NSG mice. Intraperitoneal injection of STF-083010 alone (day 1, day 8) significantly inhibits the growth of these tumors. STF-083010 is an IRE1α-specific inhibitor. Four pancreatic cancer cell lines (Panc0403, Panc1005, BxPc3, MiaPaCa2) are treated with different combination of Bortezomib (10 or 50 nM) and STF (10 or 50 μM). The normalized isobologram analysis demonstrates synergistic activity between 10 μM STF and either 10 or 50 nM bortezomib in all four cell lines. Moreover, a higher concentration of STF (50 μM) attains synergy after addition of bortezomib either at a concentration of 10 nM when tested against BxPc3 cells, at a concentration of 50 nM against Panc1005 cells, and at either 10 or 50 nM against Panc0403 cells[2]. STF-083010 (50 μM) suppresses the growth of p53-deficient human cancer cells. |
| 体内研究： |
Treatment with STF-083010 reduces the viability of HCT116 p53-/- cells by approximately 20% compared with that of HCT116 p53-/-cells. Administration of STF-083010 to tumors induced by HCT116 p53-/- cells significantly reduces tumor volume and weight by 75% and 73% at the endpoint, respectively。 |
| 参考文献： |
1. Papandreou I, et al. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. Blood. 2011 Jan 27;117(4):1311-4. 2. Chien W, et al. Selective inhibition of unfolded protein response induces apoptosis in pancreatic cancer cells. Oncotarget. 2014 Jul 15;5(13):4881-94. 3. Namba T, et al. Loss of p53 enhances the function of the endoplasmic reticulum through activation of the IRE1α/XBP1 pathway. Oncotarget. 2015 Aug 21;6(24):19990-20001. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.151 ml |
15.754 ml |
31.508 ml |
| 5 mM |
0.63 ml |
3.151 ml |
6.302 ml |
| 10 mM |
0.315 ml |
1.575 ml |
3.151 ml |
| 50 mM |
0.063 ml |
0.315 ml |
0.63 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
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京