YS3074
YS3074 is a selective ENPP1 inhibitor with an IC50 of 4.23 nM. YS3074 inhibits ENPP1-mediated hydrolysis of extracellular cGAMP, thereby preserving cGAMP to activate the STING signaling pathway. YS3074 exhibits antitumor effects both as a single agent and in combination with anti-PD-1 antibodies, enhancing tumor growth inhibition and prolonging survival. YS3074 can be used for research on colorectal cancer.
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- Fòrmula: C25H23F3N5O4P
- Peso molecular:545.45
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
60.4 nM
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Inhibition of cellular ENPP1 activity in human MDA-MB-231 cells using thymidine-5′-monophosphate p-nitrophenyl ester as substrate after 60 min incubation measured by absorbance at 405 nm.
Inhibition of cellular ENPP1 activity in human MDA-MB-231 cells using thymidine-5′-monophosphate p-nitrophenyl ester as substrate after 60 min incubation measured by absorbance at 405 nm.
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42648057 |
| CHO-K1 | IC50 |
>30 μM
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Inhibition of hERG current in CHO-K1 cells transfected with hERG measured by whole-cell patch-clamp with IC50 >30 μM.
Inhibition of hERG current in CHO-K1 cells transfected with hERG measured by whole-cell patch-clamp with IC50 >30 μM.
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42648057 |
In Vitro
YS3074 (pre-incubation for 10 min followed by enzymatic reaction for 60 min) inhibits cellular ENPP1 activity in MDA-MB-231 cells with an IC50 of 60.4 nM[1].
YS3074 (24 h) did not show significant cytotoxicity in THP-1, THP1-Blue ISG, and THP1-Dual KO-STING cells[1].
YS3074 (1-30 μM) weakly inhibits hERG currents in CHO-K1 cells, with an IC50 >30 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human THP-1-derived macrophages and murine RAW 264.7 macrophages
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Concentration:YS3074 serial dilutions (maximum final concentration 10 μM); cGAMP 2 μM (THP-1) or 5 μM (RAW 264.7); PMA 100 nM
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Incubation Time:12 h (initial incubation); 1 h (YS3074 preincubation); indicated time points (collection)
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Result:Enhanced cGAMP-induced mRNA expression of IFNB1, CXCL10, and IL6 in a dose-dependent manner.
In time-course experiments, YS3074 produced stronger and longer-lasting STING target gene expression.
No obvious cytotoxicity was observed within the tested concentration range.
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Cell Line:THP-1, THP1-Blue ISG, and THP1-Dual KO-STING cells
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Concentration:YS3074 serial dilutions; PMA 100 nM
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Incubation Time:12 h (PMA differentiation); 24 h (YS3074 incubation)
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Result:Did not show obvious cytotoxicity within the tested concentration range.
In Vivo
YS3074 (40 mg/kg; i.p.; daily) combined with anti-PD-1 antibody produces up to 73% tumor growth inhibition and prolongs survival in the CT-26 subcutaneous BALB/c mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old)[1]
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Dosage:15 mg/kg; 40 mg/kg
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Administration:i.p.; daily
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Result:Monotherapy at 40 mg/kg achieved a tumor growth inhibition rate of 40% in the CT-26 subcutaneous tumor model.
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Animal Model:BALB/c (female, 6-8 weeks old)[1]
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Dosage:15 mg/kg; 40 mg/kg
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Administration:i.p.; daily; anti-PD-1 antibody i.p. every other day
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Result:In combination with anti-PD-1 antibody, YS3074 at 15 mg/kg achieved a tumor growth inhibition rate of 48%, and at 40 mg/kg achieved a tumor growth inhibition rate of 73%, in the CT-26 subcutaneous tumor model.
Mouse survival was prolonged.
Chemical Information
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Peso molecular 545.45
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Fòrmula C25H23F3N5O4P
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SMILES
FC(C=CC=C1F)=C1C2=NC(C(NC3=CC(F)=CC=C3N4CCC(CP(O)(O)=O)CC4)=O)=CN5C2=NC=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YS3074 Related Classifications
HY-189632 Related Classifications
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