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diABZI STING agonist-1 (Tautomerism)

CAS号

2138498-18-5

分子式

C42H51N13O7

主要靶点

STING

仅限科研使用

Cat No : CM10450

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Synonyms

diABZI STING agonist-1|diABZI STING agonist|diABZI STING agonist (Compound 3)|Compound 3|STING|Tautomerism

验证数据展示

  • CAS No.: 2138498-18-5

    diABZI STING agonist-1 (Tautomerism)
    CAS#: 2138498-18-5

产品信息

CAS号 2138498-18-5
分子式 C42H51N13O7
主要靶点 STING
主要通路 免疫与炎症
分子量 849.94
纯度 99.72%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | Shipping with blue ice.
别名 diABZI STING agonist-1|diABZI STING agonist|diABZI STING agonist (Compound 3)|Compound 3|STING|Tautomerism

靶点活性

STNG (human, PBMCs):130 nM (EC50)

体内活性

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]。

体外活性

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]。

溶解度

DMSO:100 mg/mL (117.66 mM)

参考文献

1.Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7.

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