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diABZI STING agonist-1(Tautomerism)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
diABZI STING agonist-1(Tautomerism)图片
CAS NO:2138498-18-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
diABZI STING agonist-1 Tautomerism (compound 3) 是一个选择性的干扰素基因刺激受体(STING)的激动剂,其在人和小鼠中的EC50值分别为 130 nM 和 186 nM。。
生物活性

diABZISTINGagonist-1 Tautomerism (compound 3) is a selective stimulator of interferon genes(STING)receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

IC50& Target

EC50: 130 nM (human STNG in PBMCs)[1].

体外研究
(In Vitro)

diABZI STING agonist-1 (Tautomerism) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested[1].

体内研究
(In Vivo)

diABZI STING agonist-1 (Tautomerism) (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo[1].
diABZI STING agonist-1 (Tautomerism) (intravenous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (200 ng/ml)[1].
diABZI STING agonist-1 (Tautomerism) (intravenous injection; 1.5 mg/kg; 43 days) results in significant tumour growth inhibition and significantly improves survival (P < 0.001) with 8 out of 10 mice remaining tumor free at the end of the study on day 43[1].

Animal Model:Wild and Sting–/–C57Blk6 mice
Dosage:2.5 mg/kg
Administration:Subcutaneous injection; 2.5 mg/kg
Result:Activated secretion of IFNβ, IL-6, TNF, and CXCL1 in wild-type but not Sting–/–mice.
Animal Model:Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice[1]
Dosage:3 mg/kg
Administration:Intravenous injection; 3 mg/kg
Result:Exhibited a half-life of 1.4 hours and achieved systemic concentrations greater than EC50 for mouse STING (200 ng/ml).
Animal Model:Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice[1]
Dosage:1.5 mg/kg
Administration:Intravenous injection; 1.5 mg/kg; 43 days
Result:Resulted in significant tumour growth inhibition and improved survival.
分子量

849.94

Formula

C42H51N13O7

CAS 号

2138498-18-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.