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

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.

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STING agonist-46

STING agonist-46 Chemical Structure

CAS No. : 3033532-05-4

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Description

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].

In Vitro

STING agonist-46 (Compound 57) (0.37-30 μM, 24 h) exhibits potent activation on ISG pathway in THP1-Dual cells, with EC50 of 2.55 μM[1].
STING agonist-46 (10-50 μM, 24 h) shows potent activation on h-STING in THP1-Blue-ISG cells and m-STING in RAW-Lucia cells[1].
STING agonist-46 (3.3-30 μM, 2 h) significantly promotes phosphorylation of TBK1 and IRF3 in THP1-Dual cells[1].
STING agonist-46 (1.1-30 μM, 24 h) upregulates the expression of IFN-β and IP-10 in THP1-Dual cells[1].
STING agonist-46 (3.3-30 μM, 48 h) activates both hSTING-R232 and hSTING-H232 subtypes in 293T-Dual reporter cells[1].

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

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.
In Vivo

STING agonist-46 (Compound 57) (500 μg/mouse, intratumoral injection or 100 mg/kg, p.o., days 1, 4, 7) demonstrates significant anti-tumor efficacy against B16F10/CT26/4T1 melanoma in immunocompetent mice and shows no anti-tumor efficacy against B16F10/CT26 melanoma in STING-knockout mice[1].

MedChemExpress (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.
Molecular Weight

351.42

Formula

C17H21NO5S

CAS No.
SMILES

O=C(CCC(ONC(C)C)=O)C1=CC2=CC(OC)=C(C=C2S1)OC

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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.

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STING agonist-46
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HY-175714
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