1. Immunology/Inflammation
  2. STING
  3. Dazostinag disodium

Dazostinag disodium  (Synonyms: TAK-676)

目录号: HY-148029
产品使用指南

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。

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Dazostinag disodium Chemical Structure

Dazostinag disodium Chemical Structure

CAS No. : 2553413-93-5

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1 mg ¥20000
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Other Forms of Dazostinag disodium:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

STING, Type I interferons[1]

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.
Not induced the phosphorylation of pTBK1 (S172) or pIRF3 (S396) in the absence of STING expression.
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice bearing A20 syngeneic tumors/CT26.WT syngeneic tumors model[1]
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.
Clinical Trial
分子量

754.48

Formula

C21H20F2N8Na2O10P2S2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

Dazostinag disodium 相关分类

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Dazostinag disodium
目录号:
HY-148029
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