2. Immunology/Inflammation
  3. STING
  4. STING agonist-46

STING agonist-46 是一种具有口服活性的 STING 激动剂。STING agonist-46 可激活 STING 信号通路，促进 TBK1 和 IRF3 的磷酸化，并促进 IFN-β 和 IP-10 的分泌。STING agonist-46 能直接与 STING 结合并提高其热稳定性。在 B16F10、CT26 和 4T1 小鼠模型中，STING agonist-46 表现出强效的抗肿瘤功效。STING agonist-46 可用于癌症免疫治疗研究。

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STING agonist-46

STING agonist-46 Chemical Structure

CAS No. : 3033532-05-4

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STING agonist-46 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STING agonist-46 is an orally active STING agonist. STING agonist-46 activates the STING signaling pathway, promoting phosphorylation of TBK1 and IRF3, and secretion of IFN-β and IP-10. STING agonist-46 directly binds to STING and increases its thermal stability. STING agonist-46 demonstrates potent anti-tumor efficacy in B16F10, CT26, and 4T1 mouse models. STING agonist-46 can be used for cancer immunotherapy studies[1].

体外研究
(In Vitro)

STING agonist-46 (Compound 57) (0.37-30 μM, 24 h) 在 THP1-Dual 细胞中对 ISG 通路表现出强效激活作用，其EC50 为 2.55 μM[1]。
STING agonist-46 (10-50 μM, 24 h) 在 THP1-Blue-ISG 细胞中对人源 STING，在 RAW-Lucia 细胞中对鼠源 STING 均表现出强效激活作用[1]。
STING agonist-46 (3.3-30 μM, 2 h) 在 THP1-Dual 细胞中显著促进 TBK1 和 IRF3 的磷酸化[1]。
STING agonist-46 (1.1-30 μM, 24 h) 在 THP1-Dual 细胞中上调 IFN-β 和 IP-10 的表达[1]。
STING agonist-46 (3.3-30 μM, 48 h) 在 293T-Dual 报告细胞中可激活 hSTING-R232 和 hSTING-H232 两种亚型[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

STING agonist-46 相关抗体:

Cell Viability Assay[1]

Cell Line: THP1-Dual cells
Concentration: 1.1, 3.3, 10, 30 μM
Incubation Time: 24 h
Result: Upregulated the expression of IFN-β and IP-10 in THP1-Dual cells.
体内研究
(In Vivo)

STING agonist-46 (Compound 57) (500 μg/只，瘤内注射；或 100 mg/kg，口服，于第 1、4、7 天给药) 在免疫健全小鼠中，对 B16F10、CT26、4T1 肿瘤表现出显著的抗肿瘤功效；而在 STING 基因敲除小鼠中，对 B16F10、CT26 肿瘤无抗肿瘤功效[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B16F10 melanoma cells (0.5 × 105 in PBS)/CT26 colon tumor cells (2.5 × 105 in PBS)/4T1 breast cancer cells were subcutaneously implanted into the right axilla of 6-week-old female immunocompetent WT C57BL/6 mice or STING-knockout C57BL/6 mice[1]
Dosage: 500 μg/mouse, intratumoral injection or 100 mg/kg, p.o.
Administration: On days 1, 4, 7
Result: Demonstrated significant anti-tumor efficacy against B16F10/CT26/4T1 melanoma in immunocompetent mice.
Showed no anti-tumor efficacy against B16F10/CT26 melanoma in STING-knockout mice.
Showed no significant changes in body weight.
分子量

351.42

Formula

C17H21NO5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

STING agonist-46 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STING agonist-463033532-05-4STING agonist46STING agonist 46STINGStimulator of Interferon GenesTMEM173MITAERISMPYScancerB16F10CT264T1TBK1IRF3Inhibitorinhibitorinhibit

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STING agonist-46
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