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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- CAS No.: 3058842-90-0
- Formule: C20H14ClN3O4
- Masse moléculaire:395.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
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.
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Cell Line:THP1-Dual cells, THP1-STING^KO^ cells
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Concentration:12.5, 25 and 50 μM
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Incubation Time:3 h
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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.
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Cell Line:THP1-Dual cells
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Concentration:20, 30 and 40 μM (3 h incubation); 30 μM (1, 3, 6, 12 h incubation)
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Incubation Time:1, 3, 6, 12 h (30 μM); 3 h (20, 30, 40 μM)
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female; subcutaneous MC38 colorectal carcinoma model)[1]
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Dosage:10 mg/kg (i.p.); 20 mg/kg (i.p.); 50 mg/kg (p.o.); 100 mg/kg (p.o.)
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Administration:i.p.; days 1, 3, 5, 8; p.o.; days 1, 3, 5, 8
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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).
Chemical Information
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CAS No. 3058842-90-0
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Masse moléculaire 395.80
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Formule C20H14ClN3O4
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SMILES
O=C(C1=C(OC(CN2CC3=CC=CN(N=C4)C3=C4C2=O)=C5Cl)C5=CC(C)=C1)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STING agonist-50 Related Classifications
HY-181484 Related Classifications
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