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

Dazostinag disodium  (Synonyms: TAK-676)

製品番号: HY-148029 純度: 98.65%
COA 取扱説明書 Technical Support

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

Dazostinag disodium 構造式

CAS 番号 : 2553413-93-5

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
USD 6606 在庫あり
Solution
10 mM * 1 mL in Water USD 6606 在庫あり
Solid
100 μg $600 在庫あり
500 μg $1250 在庫あり
1 mg $2000 在庫あり
5 mg $3980 在庫あり
10 mg $6200 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

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製品説明

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]

体外実験

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.

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.
体内実験

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.
臨床実験
分子量

754.48

分子式

C21H20F2N8Na2O10P2S2

CAS 番号
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+]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, sealed storage, away from moisture

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

溶剤 & 溶解度
体外: 

H2O : ≥ 100 mg/mL (132.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3254 mL 6.6271 mL 13.2542 mL
5 mM 0.2651 mL 1.3254 mL 2.6508 mL
10 mM 0.1325 mL 0.6627 mL 1.3254 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

一般には略語で表示されます:C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.3254 mL 6.6271 mL 13.2542 mL 33.1354 mL
5 mM 0.2651 mL 1.3254 mL 2.6508 mL 6.6271 mL
10 mM 0.1325 mL 0.6627 mL 1.3254 mL 3.3135 mL
15 mM 0.0884 mL 0.4418 mL 0.8836 mL 2.2090 mL
20 mM 0.0663 mL 0.3314 mL 0.6627 mL 1.6568 mL
25 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3254 mL
30 mM 0.0442 mL 0.2209 mL 0.4418 mL 1.1045 mL
40 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8284 mL
50 mM 0.0265 mL 0.1325 mL 0.2651 mL 0.6627 mL
60 mM 0.0221 mL 0.1105 mL 0.2209 mL 0.5523 mL
80 mM 0.0166 mL 0.0828 mL 0.1657 mL 0.4142 mL
100 mM 0.0133 mL 0.0663 mL 0.1325 mL 0.3314 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Molarity Calculator

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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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製品名:
Dazostinag disodium
製品番号:
HY-148029
数量:
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