Description | diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. |
In vitro | diABZI STING agonist-1 (Tautomerism) 是一种选择性干扰素基因(STING)受体激动剂,对人类及小鼠的EC50分别为130 nM和186 nM。在1 μM浓度下,diABZI STING agonist-1 (Tautomerism)对测试的350多种激酶表现出高度选择性[1]。 |
In vivo | diABZI STING激动剂-1(异构体)(皮下注射;2.5 mg/kg)能够在体内诱导STING依赖性I型干扰素及促炎细胞因子的激活。diABZI STING激动剂-1(异构体)(静脉注射;3 mg/kg)表现出半衰期为1.4小时的全身暴露,并达到比STING在小鼠中的半最大有效浓度(EC50 200 ng/kg)高一半的系统浓度。diABZI STING激动剂-1(异构体)(静脉注射;1.5 mg/kg;43天)显著抑制肿瘤生长并显著提高生存率(P <0.001),其中8/10小鼠实现无肿瘤状态[1]。 |
Target activity | STNG (human, PBMCs):130 nM (EC50) |
Synonyms | diABZI STING agonist (Compound 3) |
molecular weight | 849.94 |
Molecular formula | C42H51N13O7 |
CAS | 2138498-18-5 |
Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: < 1mg/ml (insoluble), Sonication is recommended. |
References | 1. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7. |