1. Immunology/Inflammation
  2. STING
  3. TAK-676

TAK-676 

Cat. No.: HY-148029
Handling Instructions

TAK-676 is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. TAK-676 is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. TAK-676 promotes durable IFN-dependent antitumor immunity.

For research use only. We do not sell to patients.

TAK-676 Chemical Structure

TAK-676 Chemical Structure

CAS No. : 2553413-93-5

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Description

TAK-676 is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. TAK-676 is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. TAK-676 promotes durable IFN-dependent antitumor immunity[1].

IC50 & Target

STING, Type I interferons[1]

In Vitro

TAK-676 (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].
TAK-676 (0-1 μM; 24 h) exerts in vitro immune cell activation function in mouse BM-derived dendritic cells in a dose-dependent manner[1].
TAK-676 (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.
In Vivo

TAK-676 (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].
TAK-676 (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
Molecular Weight

754.48

Formula

C21H20F2N8Na2O10P2S2

CAS No.
SMILES

O[[email protected]]1[[email protected]](O[[email protected]]([S-])(OC[[email protected]](O[[email protected]](N2C3=NC=NC(N)=C3N=C2)([H])[[email protected]@H]4F)([H])[[email protected]@]4([H])O5)=O)([H])[[email protected]@](N6C(NC=NC7=O)=C7C(F)=C6)([H])O[[email protected]]1([H])CO[[email protected]]5([S-])=O.[Na+].[Na+]

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Room temperature in continental US; may vary elsewhere.

Storage

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

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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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TAK-676
Cat. No.:
HY-148029
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