diABZI STING agonist (Compound 3)

Catalog No.S8796 Batch:S879603

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Technical Data

Formula

C42H51N13O7
Molecular Weight 849.95 CAS No. 2138498-18-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (117.65 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    SUIT2 and CFPAC1 cells

  • Concentrations

    1 µM

  • Incubation Time

    72 h

  • Method

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

[1]
  • Animal Models

    BALB/c mice

  • Dosages

    3 mg/kg

  • Administration

    IV

Selleck's diABZI STING agonist (Compound 3) has been cited by 27 publications

A TBK1-independent primordial function of STING in lysosomal biogenesis [ Mol Cell, 2024, 84(20):3979-3996.e9] PubMed: 39423796
Branched glycopolymer prodrug-derived nanoassembly combined with a STING agonist activates an immuno-supportive status to boost anti-PD-L1 antibody therapy [ Acta Pharm Sin B, 2024, 14(5):2194-2209] PubMed: 38799622
TBK1-Zyxin signaling controls tumor-associated macrophage recruitment to mitigate antitumor immunity [ EMBO J, 2024, 10.1038/s44318-024-00244-9] PubMed: 39304793
Merkel cell polyomavirus protein ALTO modulates TBK1 activity to support persistent infection [ PLoS Pathog, 2024, 20(7):e1012170] PubMed: 39074144
Up-regulation of HSP90α in HDM-induced asthma causes pyroptosis of airway epithelial cells by activating the cGAS-STING-ER stress pathway [ Int Immunopharmacol, 2024, 131:111917] PubMed: 38527402
The combination of Tanshinone IIA and Astragaloside IV attenuates myocardial ischemia-reperfusion injury by inhibiting the STING pathway [ Chin Med, 2024, 19(1):34] PubMed: 38419127
Micronucleus is not a potent inducer of the cGAS/STING pathway [ Life Sci Alliance, 2024, 7(4)e202302424] PubMed: 38307626
STING guides the STX17-SNAP29-VAMP8 complex assembly to control autophagy [ Cell Insight, 2024, 3(2):100147] PubMed: 38344386
STING agonist-loaded, CD47/PD-L1-targeting nanoparticles potentiate antitumor immunity and radiotherapy for glioblastoma [ Nat Commun, 2023, 14(1):1610] PubMed: 36959214
Executioner caspases restrict mitochondrial RNA-driven Type I IFN induction during chemotherapy-induced apoptosis [ Nat Commun, 2023, 14(1):1399] PubMed: 36918588

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.