1. Immunology/Inflammation
  2. STING
  3. diABZI STING agonist-1 trihydrochloride

diABZI STING agonist-1 trihydrochloride 

Cat. No.: HY-112921B Purity: 99.89%
Handling Instructions

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.

For research use only. We do not sell to patients.

diABZI STING agonist-1 trihydrochloride Chemical Structure

diABZI STING agonist-1 trihydrochloride Chemical Structure

CAS No. : 2138299-34-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 791 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target

STING[1].

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[1].

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[1].
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)[1].
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[1].

Animal Model: Wild and Sting−/− C57Blk6 mice[1]
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

959.32

Formula

C₄₂H₅₄Cl₃N₁₃O₇

CAS No.

2138299-34-8

SMILES

O=C(N)C1=CC(N=C(NC(C2=CC(C)=NN2CC)=O)N3C/C=C/CN4C(NC(C5=CC(C)=NN5CC)=O)=NC6=C4C(OCCCN7CCOCC7)=CC(C(N)=O)=C6)=C3C(OC)=C1.[E].Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (130.30 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0424 mL 5.2120 mL 10.4241 mL
5 mM 0.2085 mL 1.0424 mL 2.0848 mL
10 mM 0.1042 mL 0.5212 mL 1.0424 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.89%

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Keywords:

diABZI STING agonist-1 trihydrochlorideSTINGStimulator of Interferon GenesTMEM173MITAERISMPYSInhibitorinhibitorinhibit

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diABZI STING agonist-1 trihydrochloride
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