中文名 | STF 083010 |
英文名 | STF 083010 |
别名 | STF-083010游离态 IRE1抑制剂(STF-083010) N-[(2-羟基-1-萘基)亚甲基]-2-噻吩磺酰胺 |
英文别名 | CS-2901 CS-2595 STF083010 STF 083010 STF-083010 N-[(2-Hydroxy-1-naphthalenyl)methylene]-2-thiophenesulfonamide 2-Thiophenesulfonamide, N-[(2-hydroxy-1-naphthalenyl)methylene]- (E)-N-((2-hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide |
CAS | 307543-71-1 |
化学式 | C15H11NO3S2 |
分子量 | 317.38 |
密度 | 1.40±0.1 g/cm3(Predicted) |
熔点 | 199-201°C |
沸点 | 548.4±56.0 °C(Predicted) |
溶解度 | DMSO: 可溶解5mg/mL (澄清溶液) |
酸度系数 | 7.31±0.50(Predicted) |
存储条件 | -20°C |
稳定性 | 从提供的购买之日起稳定1年。在DMSO中的溶液可以在-20 ° 储存长达3个月。 |
外观 | 粉末 |
颜色 | light yellow to yellow-green |
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. 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. |
危险品标志 | Xn - 有害物品 |
风险术语 | 22 - 吞食有害。 |
WGK Germany | 3 |
参考资料 展开查看 | 1: Tang ZH, Su MX, Guo X, Jiang XM, Jia L, Chen X, Lu JJ. Increased expression of IRE1α associates with the resistant mechanism of osimertinib (AZD9291)-resistant non-small cell lung cancer HCC827/OSIR cells. Anticancer Agents Med Chem. 2017 Jul 19. doi: 10.2174/1871520617666170719155517. [Epub ahead of print] PubMed PMID: 28730963. 2: Liu Y, Jiang ZY, Zhou YL, Qiu HH, Wang G, Luo Y, Liu JB, Liu XW, Bu WQ, Song J, Cui L, Jia XB, Feng L. β-elemene regulates endoplasmic reticulum stress to induce the apoptosis of NSCLC cells through PERK/IRE1α/ATF6 pathway. Biomed Pharmacother. 2017 Sep;93:490-497. doi: 10.1016/j.biopha.2017.06.073. Epub 2017 Jun 30. PubMed PMID: 28672279. 3: Song YF, Hogstrand C, Wei CC, Wu K, Pan YX, Luo Z. Endoplasmic reticulum (ER) stress and cAMP/PKA pathway mediated Zn-induced hepatic lipolysis. Environ Pollut. 2017 Sep;228:256-264. doi: 10.1016/j.envpol.2017.05.046. Epub 2017 May 23. PubMed PMID: 28549333. 4: Wang X, Xu M, Frank JA, Ke ZJ, Luo J. Thiamine deficiency induces endoplasmic reticulum stress and oxidative stress in human neurons derived from induced pluripotent stem cells. Toxicol Appl Pharmacol. 2017 Apr 1;320:26-31. doi: 10.1016/j.taap.2017.02.009. Epub 2017 Feb 11. PubMed PMID: 28193519. |
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 |
5 mM | 0.063 ml | 0.315 ml | 0.63 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!