生物活性 | |||
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描述 | Stimulator of interferon genes (STING) is an endoplasmic reticulum signaling protein which has been demonstrated to play essential roles in antitumor immunity. SR-717 is a non-nucleotide, small-molecule STING agonist with an IC50 of 7.8 μM. Within the CD45.2+ population, SR-717 treatment resulted in a significant increase in the frequency of CD8 T cells among TILs (tumor infiltrating lymphocytes) and a decrease in the frequencies of NK cells within the draining lymphnode (dLN) and spleen. In WT C57BL/6 mice, SR-717 induced IFN-β after intraperitoneal administration in a dose-dependent manner. In WT or Stinggt/gt mice, a 30 mg/kg intraperitoneal once-per-day regimen of SR-717 for 1 week was found to maximally inhibit B16.F10 tumor growth. In C57BL/6 mice bearing B16.F10 cells, SR-717 (15 mg/kg; dosed intraperitoneally; once per day) significantly inhibited the formation of pulmonary nodules in this model of metastasis. SR-717 (30 mg/kg intraperitoneally) displayed a better level of efficacy than anti-PD-1 or anti-PD-L1 antibody therapy on reducing tumor burden and improving overall survival in the B16.F10 model[2]. | ||
作用机制 | The structure of SR-717 facilitates a binding mode in which Thr263 side chain hydroxyls from both monomers are positioned to form hydrogen-bond interactions with SR-717[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.85mL 0.57mL 0.28mL |
14.24mL 2.85mL 1.42mL |
28.47mL 5.69mL 2.85mL |
参考文献 |
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