diABZI STING agonist (Compound 3)

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

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：

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
Executioner caspases restrict mitochondrial RNA-driven Type I IFN induction during chemotherapy-induced apoptosis [ Nat Commun, 2023, 14(1):1399] PubMed: 36918588
Executioner caspases restrict mitochondrial RNA-driven Type I IFN induction during chemotherapy-induced apoptosis [ Nat Commun, 2023, 14(1):1399] PubMed: 36918588
STING agonist-loaded, CD47/PD-L1-targeting nanoparticles potentiate antitumor immunity and radiotherapy for glioblastoma [ Nat Commun, 2023, 14(1):1610] PubMed: 36959214
Pharmacological inhibition of TBK1/IKKε blunts immunopathology in a murine model of SARS-CoV-2 infection [ Nat Commun, 2023, 14(1):5666] PubMed: 37723181
Innate immune pathway modulator screen identifies STING pathway activation as a strategy to inhibit multiple families of arbo and respiratory viruses [ Cell Rep Med, 2023, 4(5):101024] PubMed: 37119814
Pharmacological inhibition of TBK1/IKKε blunts immunopathology in a murine model of SARS-CoV-2 infection [ Nat Commun, 2023, 14(1):5666] PubMed: 37723181

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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