MSA-2 dimer 是一种具有选择性和口服活性的非核苷酸STING激动剂 (Kd=145 μM),有长期抗肿瘤和免疫原活性。MSA-2 dimer 作为非共价二聚体与STING结合,其渗透率高于循环二核苷酸。
生物活性 | MSA-2 dimer is a selective, orally active non-nucleotideSTINGagonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound toSTINGas a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1]. |
IC50& Target | |
体内研究 (In Vivo) | MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1]. MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1]. MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) level in tumors[1]. MSA-2 dimer (60 mg/kg; s.c.; 4 hours) concentrations is observed in tumors than in plasma or other nontumor tissues[1]. MSA-2 dimer (THP-1 cells) induces phosphorylation of both TBK1 and IR. MSA-2 dimer (10 μM and 33 μM; macrophages) induces IFN-β[1]. MSA-2 dimer also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes[1].
Animal Model: | B16F10 tumor-bearing mice | Dosage: | 60 mg/kg | Administration: | P.o.; 50 days | Result: | Inhibited tumor growth and prolonged overall survival. |
Animal Model: | C57BL6 mice | Dosage: | 40 mg/kg | Administration: | S.c.; 25 days | Result: | Induced complete tumor regression. |
Animal Model: | C57BL6 mice | Dosage: | 60 mg/kg | Administration: | P.o.; 4 hours | Result: | Increased proinflammatory cytokine (IFN-β) level in tumors. |
Animal Model: | C57BL6 mice | Dosage: | 50 mg/kg | Administration: | S.c.; 4 hours | Result: | MSA-2 concentrations were observed in tumors than in plasma or other nontumor tissues. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
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 : 70 mg/mL(123.10 mM;Need ultrasonic) 配制储备液 1 mM | 1.7585 mL | 8.7926 mL | 17.5852 mL | 5 mM | 0.3517 mL | 1.7585 mL | 3.5170 mL | 10 mM | 0.1759 mL | 0.8793 mL | 1.7585 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: ≥ 1.75 mg/mL (3.08 mM); Clear solution
此方案可获得 ≥ 1.75 mg/mL (3.08 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 17.5 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% (20%SBE-β-CDin saline) Solubility: 1.75 mg/mL (3.08 mM); Suspended solution; Need ultrasonic
此方案可获得 1.75 mg/mL (3.08 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 17.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.75 mg/mL (3.08 mM); Clear solution
此方案可获得 ≥ 1.75 mg/mL (3.08 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 17.5 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。
|