Dazostinag  (Synonyms: TAK-676 free base)

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].

Dazostinag (ADC-1, linker-payload) (121 μM; 10 min-24 hr) exhibits an half-life (t_1/2) 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.

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.

710.52

C₂₁H₂₂F₂N₈O₁₀P₂S₂

2553413-86-6

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• [1]. Ishii Yumiko, et al. Antibody drug conjugates comprising STING modulators: World Intellectual Property Organization, WO2020229982. 2020-11-19.

  [2]. WHO Drug Information-World Health Organization (WHO).