diABZI STING agonist-1 trihydrochloride

SKU: orb1220974

Description

diABZI STING agonist-1 (trihydrochloride) is stimulator of interferon genes (STING) receptor agonist.(In Vitro):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.(In Vivo):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.

Key Properties

• CAS Number: 2138299-34-8
• MW: 959.32
• Purity: >98% (HPLC)
• Formula: C₄₂H₅₄Cl₃N₁₃O₇
• SMILES: Cl.Cl.Cl.CCn1nc(C)cc1C(=O)Nc1nc2cc(cc(OC)c2n1C\C=C\Cn1c(NC(=O)c2cc(C)nn2CC)nc2cc(cc(OCCCN3CCOCC3)c12)C(N)=O)C(N)=O
• Target: STING
• Solubility: DMSO:125 mg/mL (130.30 mM)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

STING