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diABZI STING agonist-1 trihydrochloride 是选择性的干扰素基因刺激受体(STING)激动剂,在人和小鼠中都能发挥作用,其 EC50值分别为 130 和 186 nM。
diABZI STING agonist-1 trihydrochloride 是选择性的干扰素基因刺激受体(STING)激动剂,在人和小鼠中都能发挥作用,其 EC50值分别为 130 和 186 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,420 | 现货 | |
5 mg | ¥ 2,880 | 现货 | |
10 mg | ¥ 4,890 | 现货 | |
25 mg | ¥ 7,470 | 现货 | |
50 mg | ¥ 9,870 | 现货 | |
100 mg | ¥ 13,500 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 5,160 | 现货 |
产品描述 | diABZI STING agonist-1 (trihydrochloride) is stimulator of interferon genes (STING) receptor agonist. |
体外活性 | diABZI STING agonist-1 trihydrochloride 是选择性的干扰素基因刺激受体(STING)激动剂,在人和小鼠中都能发挥作用,其 EC50值分别为 130 和 186 nM。 |
体内活性 | 方法:diABZI STING agonist-1 (trihydrochloride) (3mg/kg,静脉注射 )在BALB/c小鼠体内,观察小鼠体内的药代动力学谱。 结果:diABZI STING agonist-1 (trihydrochloride) 全身性暴露,半衰期为1.4 h,全身性浓度大于小鼠STING的半最大有效浓度(EC50) (200 ng /ml)。[1] 方法:diABZI STING agonist-1 (trihydrochloride) (1.5 mg/kg, 1、4和8天,静脉注射)在皮下CT-26肿瘤的小鼠中,通过肿瘤体积AUC分析。 结果:diABZI STING agonist-1 (trihydrochloride) 对肿瘤生长有明显的抑制作用,显著提高了生存率(P<0.001)。[1] |
动物实验 | To evaluate the potential therapeutic effects of systemically administered diABZI STING agonist-1 trihydrochloride, tested the efficacy of intravenously delivered diABZI STING in a syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice.?We first established the pharmacokinetic profile of STING in BALB/c mice following intravenous injection of 3 mg/kg .?STING exhibited systemic exposure with a half-life of 1.4 h and achieved systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (~200 ng/ml).?Next, we tested an intermittent dosing paradigm in which 1.5 mg/kg STING was injected intravenously on days 1, 4, and 8 in mice with approximately 100 mm^3 subcutaneous CT-26 tumours.?Treatment with STING resulted in significant tumour growth inhibition as measured by tumour volume AUC analysis (P<0.001), and significantly improved survival (P<0.001) with 8 out of 10 mice remaining tumour free at the end of the study on day 43. |
分子量 | 959.32 |
分子式 | C42H54Cl3N13O7 |
CAS No. | 2138299-34-8 |
Smiles | Cl.Cl.Cl.CCn1nc(C)cc1C(=O)Nc1nc2cc(cc(OC)c2n1C\C=C\Cn1c(NC(=O)c2cc(C)nn2CC)nc2cc(cc(OCCCN3CCOCC3)c12)C(N)=O)C(N)=O |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 100 mg/mL (104.24 mM), Sonication is recommended. DMSO: 100 mg/mL (104.24 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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