Dazostinag,2553413-86-6

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Dazostinag

CAS No. : 2553413-86-6

MCE 国际站：Dazostinag

产品活性：Dazostinag (TAK-676 free base) 是干扰素基因刺激剂 (STING) 蛋白的激动剂，具有抗肿瘤活性。Dazostinag 可作为有效载荷 (playload) 用于合成抗体偶联活性分子 (ADC)。

研究领域：Immunology/Inflammation

作用靶点：STING

In Vitro: 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.
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.
Dazostinag (ADC-1) (10 μg/mL; 0-96 hr) shows plasma stability in human, primate and mouse plasma.

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.
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.

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