2. Immunology/Inflammation NF-κB GPCR/G Protein
  3. STING IKK IFNAR Interleukin Related CXCR
  4. STING agonist-50

STING agonist-50 is an orally active STING agonist with an IC50 of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer.

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STING agonist-50

STING agonist-50 Chemical Structure

CAS No. : 3058842-90-0

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STING agonist-50 Related Antibodies

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Description

STING agonist-50 is an orally active STING agonist with an IC50 of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

TBK1

 

IL-6

 

In Vitro

STING agonist-50 (Compound X41) activates the STING signaling pathway in THP1-Dual cells, with EC50 values of 13.60 μM for IRF3-driven luciferase activity and 17.52 μM for NF-κB-driven luciferase activity[1].
STING agonist-50 (12.5-50 μM; 3 h) induces concentration-dependent upregulation of IFN-β, CXCL10, and IL-6 mRNA in THP1-Dual cells via a STING-dependent mechanism, with no effect on IFN-β mRNA in STING-knockout THP1 cells[1].
STING agonist-50 (20-40 μM; 1-12 h) induces time-dependent and concentration-dependent phosphorylation of STING, TBK1, and IRF3 in THP1-Dual cells, with maximal activation observed at 3 h post-treatment[1].

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

STING agonist-50 Related Antibodies

Real Time qPCR[1]

Cell Line: THP1-Dual cells, THP1-STING^KO^ cells
Concentration: 12.5, 25 and 50 μM
Incubation Time: 3 h
Result: Induced concentration-dependent upregulation of IFN-β, CXCL10, and IL-6 mRNA in THP1-Dual cells.
Did not increase IFN-β mRNA transcription in THP1-STING^KO^ cells even at 50 μM.

Western Blot Analysis[1]

Cell Line: THP1-Dual cells
Concentration: 20, 30 and 40 μM (3 h incubation); 30 μM (1, 3, 6, 12 h incubation)
Incubation Time: 1, 3, 6, 12 h (30 μM); 3 h (20, 30, 40 μM)
Result: Induced maximal phosphorylation of STING, TBK1, and IRF3 at 3 h post-treatment.
Promoted phosphorylation of these downstream proteins in a concentration-dependent manner.
Parmacokinetics
Species Dose Route AUCINF_obs T1/2 Vz CL Tmax Cmax F
Rat[1] 1 mg/kg i.v. 72.91 μg·h/mL 4.43 h 87.78 mL/kg 0.23 mL/min/kg / / /
Rat[1] 5 mg/kg i.p. 141.42 μg·h/mL 4.11 h 209.71 mL/kg 0.59 mL/min/kg 0.26 h 82.37 μg/mL 39.57 %
Rat[1] 8 mg/kg p.o. 60.08 mg·h/L 9.92 h 1904.93 mL/kg 2.24 mL/min/kg 0.33 h 8.32 μg/mL 10.51 %
In Vivo

STING agonist-50 (Compound X41) (10-100 mg/kg; i.p., p.o.; days 1, 3, 5, 8) exhibits potent dose-dependent antitumor efficacy in a mouse MC38 colorectal carcinoma model[1].

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

Animal Model: C57BL/6 (female; subcutaneous MC38 colorectal carcinoma model)[1]
Dosage: 10 mg/kg (i.p.); 20 mg/kg (i.p.); 50 mg/kg (p.o.); 100 mg/kg (p.o.)
Administration: i.p.; days 1, 3, 5, 8; p.o.; days 1, 3, 5, 8
Result: Achieved complete tumor regression in 2 out of 6 mice (10 mg/kg i.p.).
Achieved complete tumor regression in 3 out of 6 mice, and drastically reduced final tumor volumes and weights relative to controls (20 mg/kg i.p.).
Significantly reduced final tumor volumes and weights compared to saline controls, with robust tumor growth inhibition and no complete regression (50 mg/kg p.o.).
Significantly reduced final tumor volumes and weights compared to saline controls (100 mg/kg p.o.).
Showed no significant body weight changes relative to controls, indicating good tolerability (all doses).
Induced significantly higher plasma IFN-β levels 4 hours post-administration than 10 mg/kg Compound 22 (10 mg/kg i.p.).
Induced measurable plasma IFN-β levels (50 mg/kg p.o.).
Caused no significant histopathological alterations in kidney, lung, spleen, liver, and heart tissue (all doses).
Molecular Weight

395.80

Formula

C20H14ClN3O4
CAS No.
SMILES

O=C(C1=C(OC(CN2CC3=CC=CN(N=C4)C3=C4C2=O)=C5Cl)C5=CC(C)=C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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STING agonist-50 Related Classifications

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Help & FAQs
  • 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-503058842-90-0STING agonist50STING agonist 50STINGIKKIFNARInterleukin RelatedCXCRStimulator of Interferon GenesTMEM173MITAERISMPYSIκB kinaseI kappa B kinase Interferon-α/β receptorInterferon-alpha/beta receptor ILCXC chemokine receptorsC-X-C motif chemokine receptorsTBK1MC38 colorectal carcinomasyngeneic mouse modelsIRF3STING signaling pathwayIL-6human STINGCXCL10IFN-βTHP1-Dual cellsInhibitorinhibitorinhibit

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