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

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.

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Dazostinag disodium Chemical Structure

Dazostinag disodium Chemical Structure

CAS No. : 2553413-93-5

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Dazostinag disodium Related Antibodies

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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[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.

Dazostinag disodium Related Antibodies

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.
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].

MedChemExpress (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
Molecular Weight

754.48

Formula

C21H20F2N8Na2O10P2S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CN([C@H]2[C@H](O[P@@](OC[C@@H]3[C@@H](O4)[C@@H](F)[C@H](N5C6=NC=NC(N)=C6N=C5)O3)([S-])=O)[C@H](O)[C@@H](COP4([S-])=O)O2)C7=C1C(N=CN7)=O.[Na+].[Na+]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Dazostinag disodium Related Classifications

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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.

Keywords:

Dazostinag disodium2553413-93-5TAK-676TAK676TAK 676STINGStimulator of Interferon GenesTMEM173MITAERISMPYST-cell responsetumor microenvironmentTMEinnate immuneadaptive immunecomplete regressionsdurable memoryT-cell immunityIFN-dependentInhibitorinhibitorinhibit

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