diABZI STING agonist-1 (tautomerism)

製品コードS8796 バッチS879602

印刷

化学情報

 Chemical Structure Synonyms diABZI STING agonist-1, Tautomerism Storage
(From the date of receipt)
3 years-20°C powder
化学式

C42H51N13O7

分子量 849.95 CAS No. 2138498-18-5
Solubility (25°C)* 体外 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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 SUIT2 and CFPAC1 cells
濃度 1 µM
反応時間 72 h
実験の流れ

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

動物実験 動物モデル BALB/c mice
投薬量 3 mg/kg
投与方法 IV

参考

  • https://www.ncbi.nlm.nih.gov/pubmed/?term=30405246
  • https://pubmed.ncbi.nlm.nih.gov/35021095/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Trans-Golgi network tethering factors regulate TBK1 trafficking and promote the STING-IFN-I pathway [ Cell Discov, 2025, 11(1):23] PubMed: 40097395
Potentiating cancer immunotherapies with modular albumin-hitchhiking nanobody-STING agonist conjugates [ Nat Biomed Eng, 2025, 10.1038/s41551-025-01400-0] PubMed: 40500332
PARP7 inhibits type I interferon signaling to prevent autoimmunity and lung disease [ J Exp Med, 2025, 222(5)e20241184] PubMed: 39969510
Macromolecular Diamidobenzimidazole Conjugates Can Activate Stimulator of Interferon Genes [ J Am Chem Soc, 2025, 147(38):35149-35163] PubMed: 40939638
Dimethyl fumarate alleviate hepatic ischemia-reperfusion injury through suppressing cGAS-STING signaling [ MedComm (2020), 2025, 6(2):e70077] PubMed: 39877286
Disulfiram/copper triggers cGAS-STING innate immunity pathway via ROS-induced DNA damage that potentiates antitumor response to PD-1 checkpoint blockade [ Int J Biol Sci, 2025, 21(4):1730-1748] PubMed: 39990655
Exercise-induced adipokine Nrg4 alleviates MASLD by disrupting hepatic cGAS-STING signaling [ Cell Rep, 2025, 44(2):115251] PubMed: 39891907
Biomimetic nanovesicle vaccines derived from dendritic cells sensitized with whole tumor antigens for melanoma immunotherapy [ Mater Today Bio, 2025, 35:102409] PubMed: 41146660
Differential tropisms of old and new world hantaviruses influence virulence and developing host-directed antiviral candidates [ PLoS Pathog, 2025, 21(8):e1013401] PubMed: 40857262
AUP1 and UBE2G2 complex targets STING signaling and regulates virus-induced innate immunity [ mBio, 2025, e0060225.] PubMed: 40237449

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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