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编 号：F753686
分子式：C21H20F2N8Na2O10P2S2
分子量：754.48
分子式：C21H20F2N8Na2O10P2S2
分子量：754.48
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CAS No: 2553413-93-5
产品详情
生物活性：
Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity.
体内研究：
Dazostinag disodium (0.025-2 mg/kg; i.v.; single dose) is well tolerated, exhibits dose-proportional pharmacokinetics in plasma, and exhibits higher exposure in tumor in mice.Dazostinag disodium (1 mg/kg/d, 2 mg/kg/d; i.v.; 13 d) shows anti-tumor function on BALB/c mice bearing A20 syngeneic tumors/CT26.WT syngeneic tumors mode.Animal Model:BALB/c mice bearing A20 syngeneic tumors/CT26.WT syngeneic tumors model
Dosage:1 or 2 mg/kg/day
Administration:Intravenous injection; for 3, 6, 9, 12 day, respectively
Result:Resulted in significant T cell–dependent in vivo antitumor activity.Induced dose-dependent cytokine responses and increased the activation and proliferation of immune cells within the TME and tumor-associated lymphoid tissue.
体外研究：
Dazostinag disodium (1.1, 3.3, and 10 μM; 2 h) dose-dependently activates the STING-TBK1-IRF3 pathway in THP1-Dual human AML cells and CT26.WT cells, but is critically dependent on STING expression.Dazostinag disodium (0-1 μM; 24 h) exerts in vitro immune cell activation function in mouse BM-derived dendritic cells in a dose-dependent manner.Dazostinag disodium (0-1 μM; 24 h) promotes the activation of dendritic cells (DC), natural killer (NK) cells, and T cells, with activation EC50s of 1.27 μM (MoDC), 0.32 μM (BMDC), 0.271 μM (NK), 0.216 μM (CD8+), 0.249 μM (CD4+) at 24 h, respectively.
Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity.
体内研究：
Dazostinag disodium (0.025-2 mg/kg; i.v.; single dose) is well tolerated, exhibits dose-proportional pharmacokinetics in plasma, and exhibits higher exposure in tumor in mice.Dazostinag disodium (1 mg/kg/d, 2 mg/kg/d; i.v.; 13 d) shows anti-tumor function on BALB/c mice bearing A20 syngeneic tumors/CT26.WT syngeneic tumors mode.Animal Model:BALB/c mice bearing A20 syngeneic tumors/CT26.WT syngeneic tumors model
Dosage:1 or 2 mg/kg/day
Administration:Intravenous injection; for 3, 6, 9, 12 day, respectively
Result:Resulted in significant T cell–dependent in vivo antitumor activity.Induced dose-dependent cytokine responses and increased the activation and proliferation of immune cells within the TME and tumor-associated lymphoid tissue.
体外研究：
Dazostinag disodium (1.1, 3.3, and 10 μM; 2 h) dose-dependently activates the STING-TBK1-IRF3 pathway in THP1-Dual human AML cells and CT26.WT cells, but is critically dependent on STING expression.Dazostinag disodium (0-1 μM; 24 h) exerts in vitro immune cell activation function in mouse BM-derived dendritic cells in a dose-dependent manner.Dazostinag disodium (0-1 μM; 24 h) promotes the activation of dendritic cells (DC), natural killer (NK) cells, and T cells, with activation EC50s of 1.27 μM (MoDC), 0.32 μM (BMDC), 0.271 μM (NK), 0.216 μM (CD8+), 0.249 μM (CD4+) at 24 h, respectively.
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