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MedChemExpress - Model Dazostinag disodium - 2553413-93-5

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[1].

Dazostinag disodium

MCE China：Dazostinag disodium

Brand：MedChemExpress (MCE)

Cat. No.HY-148029

CAS：2553413-93-5

Synonyms：TAK-676

Purity：98.16%

Storage：-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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[1]. 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[1]. 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[1].

In Vivo：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[1]. 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[1].

IC50 & Target：STING, Type I interferons[1] In Vitro 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[1]. 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[1]. 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[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Dazostinag disodium Related Antibodies Western Blot Analysis[1] Cell Line: THP1-Dual human AML cells and CT26.WT cells

References：

[1]. Elizabeth CC, et al. TAK-676: A Novel Stimulator of Interferon Genes (STING) Agonist Promoting Durable IFN-dependent Antitumor Immunity in Preclinical Studies. Cancer Research Communications. 2022. 2(6): 489–502.

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