Dazostinag disodium

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Dazostinag disodium (TAK-676) 是一种干扰素基因刺激因子激动剂 (STING)，触发 STING 信号通路激活和 I 型干扰素激活。Dazostinag disodium 也是一种免疫系统调节剂，具有完全消退和持久记忆的 T 细胞免疫功能。Dazostinag disodium 能够促进持久的干扰素依赖性抗肿瘤免疫反应。

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.

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.Western Blot Analysis Cell Line:THP1-Dual human AML cells and CT26.WT cells Concentration:1.1, 3.3, 10 μM Incubation Time:2 hours Result:Increased pTBK1, pSTING, pIRF3 protein level in a dose-dependent manner.

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.

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Immunology/Inflammation

STING

STING

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2553413-93-5

754.48

C21H20F2N8Na2O10P2S2

>98% (HPLC)

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O[C@H]1[C@@]2([C@@H](O[C@@]1(COP([S-])(O[C@@]3([C@@]([H])(COP([S-])(O2)=O)O[C@H]([C@@H]3F)N4C5=NC=NC(N)=C5N=C4)[H])=O)[H])N6C7=C(C(F)=C6)C(N=CN7)=O)[H].[Na+].[Na+]

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(-20℃)

With Ice Pack

≥ 2 years