diABZI STING agonist-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

diABZI STING agonist-1 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。

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.

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.

diABZI STING agonist-1 (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo.?diABZI STING agonist-1 (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 (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.

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Immunology/Inflammation

STING

STING

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2138299-33-7

849.94

C42H51N13O7

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (117.66 mM; 超声助溶 )

O=C(C1=CC(C)=NN1CC)N=C2N(C3=C(OC)C=C(C(N)=O)C=C3N2)C/C=C/CN4C5=C(OCCCN6CCOCC6)C=C(C(N)=O)C=C5NC4=NC(C7=CC(C)=NN7CC)=O

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(-20℃)

With Ice Pack

≥ 2 years