diABZI STING agonist (Compound 3)

Synonyms: diABZI STING agonist-1, Tautomerism

diABZI STING agonist (diABZI STING agonist-1, Compound 3, Tautomerism) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans.Solutions are unstable and should be fresh-prepared.

diABZI STING agonist (Compound 3) Chemical Structure

diABZI STING agonist (Compound 3) Chemical Structure

CAS No. 2138498-18-5

Purity & Quality Control

diABZI STING agonist (Compound 3) Related Products

Biological Activity

Description diABZI STING agonist (diABZI STING agonist-1, Compound 3, Tautomerism) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans.Solutions are unstable and should be fresh-prepared.
Targets
STING [1]
In vitro
In vitro

In human PBMCs, compound 3 induces dose-dependent activation of STING and secretion of IFNβ with an EC50app of 130 nM[1].

Cell Research Cell lines SUIT2 and CFPAC1 cells
Concentrations 1 µM
Incubation Time 72 h
Method

Cells were treated with diABZI (1 µM) for 72 hr.

Experimental Result Images Methods Biomarkers Images PMID
Western blot LC3 / pIRF3 / actin 32949635
In Vivo
In vivo

Compound 3 activates secretion of IFNβ, IL-6, TNF, and KC/GROα (also known as CXCL1) in wild-type but not Sting−/− mice. In BALB/c mice administrated 3 mg/kg compound 3 via intravenous injection, compound 3 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). In mice bearing subcutaneous CT-26 tumours, treatment with compound 3 results in significant tumour growth inhibition as measured by tumour volume AUC analysis (P<0.001), and significantly improves survival (P<0.001) with 8 out of 10 mice remaining tumour free at the end of the study on day 43[1].

Animal Research Animal Models BALB/c mice
Dosages 3 mg/kg
Administration IV

Chemical Information & Solubility

Molecular Weight 849.95 Formula

C42H51N13O7

CAS No. 2138498-18-5 SDF --
Smiles CCN1C(=CC(=N1)C)C(=O)NC2=NC3=C(N2CC=CCN4C5=C(C=C(C=C5OCCCN6CCOCC6)C(=O)N)N=C4NC(=O)C7=CC(=NN7CC)C)C(=CC(=C3)C(=O)N)OC
Storage (From the date of receipt) 3 years-20°C powder Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.

In vitro
Batch:

DMSO : 100 mg/mL ( (117.65 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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