产品
编 号:F272640
分子式:C42H54Cl3N13O7
分子量:959.32
产品类型
结构图
CAS No: 2138299-34-8
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产品详情
生物活性:
diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
体内研究:
diABZI STING agonist-1 trihydrochloride (subcutaneous injection; 2.5 mg/kg)induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo.diABZI STING agonist-1 trihydrochloride (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).diABZI STING agonist-1 trihydrochloride (intravenous injection; 1.5 mg/kg; days 1, 4 and 8; 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.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
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
Dosage:1.5 mg/kg
Administration:Intravenous injection; 1.5 mg/kg; 43 days
Result:Resulted in significant tumour growth inhibition and improved survival.
体外研究:
diABZI STING agonist-1 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.