diABZI STING agonist-1 trihydrochloride

SKU: orb1689878

Description

diABZI STING agonist-1 trihydrochloride is a synthetic small molecule agonist of the STING (Stimulator of Interferon Genes) receptor. It potently activates the cGAS-STING pathway, inducing type I interferon and cytokine production, and is widely used in immuno-oncology and antiviral research in both cellular and animal models.

Research Area

Immunology & Inflammation

Images & Validation

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Key Properties

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CAS Number	2138299-34-8
MW	959.32
Purity	99.55% (May vary between batches)
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	H2O:5 mg/mL (5.21 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.08 mM);DMSO:15 mg/mL (15.64 mM)

Bioactivity

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Target IC50	STING (human):130 nM (EC50)\|STING (mouse):200 ng /mL (EC50)\|H69AR cells:0.035 μM (EC50)
In Vivo	METHODS: diABZI STING agonist-1 (trihydrochloride) (3mg/kg, intravenous injection) was administered to BALB/c mice to observe the pharmacokinetic spectrum in the mice. RESULTS diABZI STING agonist-1 (trihydrochloride) was systematically exposed, with a half-life of 1.4 h, and the systemic concentration was greater than the half-maximum effective concentration (EC50) of mouse STING (200 ng/ml). METHODS: diABZI STING agonist-1 (trihydrochloride) (1.5 mg/kg, 1, 4 and 8 days, intravenous injection) in mice with subcutaneous CT-26 tumors was analyzed by tumor volume AUC. RESULTS diABZI STING agonist-1 (trihydrochloride) had a significant inhibitory effect on tumor growth and significantly improved survival rate (P<0.001). Read more...
In Vitro	diABZI STING agonist-1 trihydrochloride is a selective stimulator of interferon genes receptor (STING) agonist with EC50 values of 130 and 186 nM in humans and mice. Read more...
Animal Research	To evaluate the potential therapeutic effects of systemically administered diABZI STING agonist-1 trihydrochloride, tested the efficacy of intravenously delivered diABZI STING in a syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice. We first established the pharmacokinetic profile of STING in BALB/c mice following intravenous injection of 3 mg/kg . STING exhibited systemic exposure with a half-life of 1.4 h and achieved systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (~200 ng/ml). Next, we tested an intermittent dosing paradigm in which 1.5 mg/kg STING was injected intravenously on days 1, 4, and 8 in mice with approximately 100 mm^3 subcutaneous CT-26 tumours. Treatment with STING resulted in significant tumour growth inhibition as measured by tumour volume AUC analysis (P<0.001), and significantly improved survival (P<0.001) with 8 out of 10 mice remaining tumour free at the end of the study on day 43. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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diABZI STING agonist 1 trihydrochloride, diABZI STING agonist-1, diABZI STING agonist1 trihydrochloride, diABZI STING agonist-1 trihydrochloride, diABZI STING agonist-1 Trihydrochloride, inhibit, MPYS, MITA, Inhibitor, ERIS, Stimulator of Interferon Genes, STING, TMEM173

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Compound Identifiers

PubChem CID

137701219 ↗

Key Properties

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No computed properties available.

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