SR-717 是一种非核苷类STING激动剂,在 ISG-THP1 (WT) 和 ISG-THP1 cGAS KO (cGAS KO) 细胞中的EC50分别为 2.1 μM 和 2.2 μM。SR-717 是一种稳定的环鸟苷单磷酸腺苷单磷酸 (cGAMP) 类似物。具有抗肿瘤活性。
生物活性 | SR-717 is a non-nucleotideSTINGagonist withEC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity[1]. |
体外研究 (In Vitro) | SR-717 activates STING by inducing the same closed conformation, which thereby provides an avenue to explore this class of systemic STING agonist in diverse contexts, including antitumor immunity[1]. SR-717 (3.8 μM) induces the expression of PD-L1 in THP1 cells and in primary human peripheral blood mononuclear cells in a STING-dependent manner[1].
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体内研究 (In Vivo) | SR-717 (30 mg/kg intraperitoneal once-per-day for 1 week) shows antitumor activities in WT orStinggt/gtmice[1]. SR-717 (30 mg/kg intraperitoneally for 7 days) displays antitumor activity; promots the activation of CD8+T, natural killer, and dendritic cells in relevant tissues; and facilitates antigen cross-priming[1].
Animal Model: | WT orStinggt/gtmice[1] | Dosage: | 30 mg/kg | Administration: | Intraperitoneally; once-per-day for 1 week | Result: | Maximally inhibited tumor growth. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 20.83 mg/mL(59.31 mM;Need ultrasonic) 配制储备液 1 mM | 2.8475 mL | 14.2373 mL | 28.4746 mL | 5 mM | 0.5695 mL | 2.8475 mL | 5.6949 mL | 10 mM | 0.2847 mL | 1.4237 mL | 2.8475 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (5.92 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (5.92 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.92 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.92 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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