2553413-86-6

2553413-86-6 structure
2553413-86-6 structure
  • Name: Dazostinag
  • Chemical Name: Dazostinag
  • CAS Number: 2553413-86-6
  • Molecular Formula: C21H22F2N8O10P2S2
  • Molecular Weight: 710.52
  • Catalog: Signaling Pathways Immunology/Inflammation STING
  • Create Date: 2023-04-25 08:17:19
  • Modify Date: 2024-04-07 10:12:40
  • 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].

Name Dazostinag
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].
Related Catalog
In Vitro Dazostinag (ADC-1,连接子-有效载荷) (121 μM;10 min-24 hr) 在大鼠肝脏三倍体中的半衰期 (t1/2) 为 2.4 小时[1]。 Dazostinag (ADC-1,连接子-有效载荷) 在具有人 STING 的 R232 变体的 THP1 细胞中激活人鸟苷酸环化酶 C (GCC),EC50 为 0.068 nM[1]。 Dazostinag (ADC-1) (10 μg/mL;0-96 小时) 在人、灵长类动物和小鼠血浆中表现出血浆稳定性[1]。
In Vivo Dazostinag (ADC-1) (0.1 mg/kg;单剂量) 在携带 CT26-GCC 肿瘤的 Balb/C 小鼠中,半衰期为 33 小时,AUC (last) 值为 51432 h·nM[1]。 Dazostinag (ADC-1) (50 μg/kg,100 μg/kg;静脉注射;单剂量,监测 2 周) 显著抑制 Balb/C 小鼠中、表达 GCC 的 CT26 结肠癌小鼠肿瘤的生长[1]。 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.
References

[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).

Molecular Formula C21H22F2N8O10P2S2
Molecular Weight 710.52