1. Immunology/Inflammation
  2. STING
  3. Dazostinag

Dazostinag (TAK-676 free base) is an agonist of stimulator of interferon genes (STING) protein with antineoplastic activity. Dazostinag can serve as a playload to synthesis antibody-drug conjugates (ADCs).

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Dazostinag disodium) that retains the same biological activity.

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

Dazostinag

Dazostinag Chemical Structure

CAS No. : 2553413-86-6

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Description

Dazostinag (TAK-676 free base) is an agonist of stimulator of interferon genes (STING) protein with antineoplastic activity. Dazostinag can serve as a playload to synthesis antibody-drug conjugates (ADCs)[1][2].

In Vitro

Dazostinag (ADC-1, linker-payload) (121 μM; 10 min-24 hr) exhibits an half-life (t1/2) of 2.4 hr in rat liver tritosomes[1].
Dazostinag (ADC-1, linker-payload) activates human Guanylyl cyclase C (GCC) with an EC50 value of 0.068 nM in THPl cells with R232 variant of human STING[1].
Dazostinag (ADC-1) (10 μg/mL; 0-96 hr) shows plasma stability in human, primate and mouse plasma[1].

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

In Vivo

Dazostinag (ADC-1) (0.1 mg/kg; single dose) shows an half-life of 33 h and the AUC (last) value of 51432 h·nM in Balb/C mice bearing CT26-GCC tumors[1].
Dazostinag (ADC-1) (50 μg/kg, 100 μg/kg; i.v.; single dose, monitored for 2 weeks) significantly inhibits the growth of tumor in Balb/C mouse bearing GCC-expressing CT26 colon carcinoma mouse tumors[1].

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

Animal Model: CT26 colon carcinoma model in female Balb/C mice (6-8 weeks old)[1]
Dosage: 50 μg/kg, 100 μg/kg
Administration: IP; single dose, monitored for 15 days, measured two times per week
Result: Significantly suppressed the volume of tumor in mice.
Molecular Weight

710.52

Formula

C21H22F2N8O10P2S2

CAS No.
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

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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.

Purity & Documentation
References
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Dazostinag 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.

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Dazostinag
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HY-152861
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