STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
IC50&Target
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 p53cells. 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.
分子式
C15H11NO3S2
分子量
317.38
CAS号
307543-71-1
运输条件
Room temperature in continental US; may vary elsewhere.