diABZI STING agonist-1(Tautomerism)

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CAS NO:

2138498-18-5

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.