中文同义词:
IRE1抑制剂(STF-083010);N-[(2-羟基-1-萘基)亚甲基]-2-噻吩磺酰胺
英文同义词:
STF-083010;STF083010;STF 083010;CS-2595;CS-2901;STF 083010;(E)-N-((2-hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide;N-[(2-Hydroxy-1-naphthalenyl)methylene]-2-thiophenesulfonamide;2-Thiophenesulfonamide, N-[(2-hydroxy-1-naphthalenyl)methylene]-
相关类别:
细胞生物学试剂;小分子抑制剂，天然产物;Inhibitors
沸点
548.4±56.0 °C(Predicted)
密度
1.40±0.1 g/cm3(Predicted)
溶解度
DMSO: soluble5mg/mL (clear solution)
酸度系数(pKa)
7.31±0.50(Predicted)
颜色
light yellow to yellow-green
生物活性
STF-083010 是一种 IRE1α 特异性抑制剂。在内质网应激后，STF-083010 抑制 Ire1 内切核酸酶活性，而不影响其激酶活性。
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.
