1. Immunology/Inflammation
  2. STING
  3. diABZI STING agonist-1 (Tautomerism)

diABZI STING agonist-1 (Tautomerism) 

Cat. No.: HY-112921
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diABZI STING agonist-1 Tautomerism (compound 3) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.

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diABZI STING agonist-1 (Tautomerism) Chemical Structure

diABZI STING agonist-1 (Tautomerism) Chemical Structure

CAS No. : 2138498-18-5

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Description

diABZI STING agonist-1 Tautomerism (compound 3) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.

IC50 & Target

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

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].

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.
Molecular Weight

849.94

Formula

C₄₂H₅₁N₁₃O₇

CAS No.

2138498-18-5

SMILES

O=C(N)C1=CC(N/C(N2C/C=C/CN3/C(NC4=C3C(OCCCN5CCOCC5)=CC(C(N)=O)=C4)=N/C(C6=CC(C)=NN6CC)=O)=N\C(C7=CC(C)=NN7CC)=O)=C2C(OC)=C1

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diABZI STING agonist-1 (Tautomerism)
Cat. No.:
HY-112921
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