SR-717

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Chemical Structure| 2375421-09-1 同义名 : SR-717 lithium;SR 717 (lithium salt)
CAS号 : 2375421-09-1
货号 : A1340104
分子式 : C15H8F2LiN5O3
纯度 : 99%+
分子量 : 351.193
MDL号 : N/A
存储条件:

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 20 mg/mL(56.95 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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

[1]Emily N Chin, et al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999.

[2]Chin EN, et al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999