YS3375
YS3375 is an ENPP1 inhibitor with an IC50 of 19.4 nM. YS3375 prevents cGAMP hydrolysis and sustains STING pathway activation. YS3375 can be used for research on colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C23H22F3N4O4P
- Molecular Weight:506.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
186 nM
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Inhibition of intracellular ENPP1 in human MDA-MB-231 breast cancer cells using thymidine-5′-monophosphate p-nitrophenyl ester as substrate after 10 min compound preincubation and 60 min reaction measuring p-nitrophenol absorbance at 405 nm.
Inhibition of intracellular ENPP1 in human MDA-MB-231 breast cancer cells using thymidine-5′-monophosphate p-nitrophenyl ester as substrate after 10 min compound preincubation and 60 min reaction measuring p-nitrophenol absorbance at 405 nm.
|
42648057 |
| CHO-K1 | IC50 |
30 μM
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Inhibition of hERG current in CHO-K1 cells transfected with hERG by whole-cell patch clamp with IC50 >30 μM.
Inhibition of hERG current in CHO-K1 cells transfected with hERG by whole-cell patch clamp with IC50 >30 μM.
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42648057 |
In Vitro
YS3375 (10 min) selectively inhibits recombinant ENPP1 with an IC50 of 19.4 nM, showing greater selectivity for ENPP1 over ENPP2 and ENPP3[1].
YS3375 (pre-incubation for 10 min; substrate reaction for 60 min) inhibits cell-associated ENPP1 in MDA-MB-231 cells with an IC50 of 186 nM[1].
YS3375 (24 h) showed no obvious cytotoxicity in THP-1, THP1-Blue ISG, or THP1-Dual KO-STING cells within 24 h[1].
YS3375 (1-30 μM) showed weak inhibition of hERG current in CHO-K1 cells, with an IC50 >30 μM[1].
YS3375 exhibited the poorest stability in monkey liver microsomes (t1/2 24.1 min)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:THP-1, THP1-Blue ISG, and THP1-Dual KO-STING cells
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Concentration:serial dilutions
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Incubation Time:24 h
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Result:Showed no obvious cytotoxicity within the tested concentration range.
In Vivo
YS3375 (40 mg/kg; intraperitoneal; daily) combined with anti-PD-1 (intraperitoneal; every other day) produces 67% TGI in the CT-26 colorectal cancer 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 to 8 weeks of age)[1]
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Dosage:40 mg/kg
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Administration:intraperitoneal; daily
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Result:Achieved a tumor growth inhibition rate of 50% at 40 mg/kg in the CT-26 colorectal cancer model.
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Animal Model:BALB/c (female, 6 to 8 weeks of age)[1]
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Dosage:40 mg/kg (YS3375); anti-PD-1 antibody
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Administration:YS3375 intraperitoneal; daily; anti-PD-1 antibody intraperitoneal; every other day
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Result:In combination with anti-PD-1 antibody, YS3375 at 40 mg/kg achieved a tumor growth inhibition rate of 67% in the CT-26 colorectal cancer model.
Chemical Information
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Molecular Weight 506.41
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Formula C23H22F3N4O4P
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SMILES
FC(C=CC=C1F)=C1C2=NC(C(NC3=CC(F)=CC=C3N4CCC(CP(O)(O)=O)CC4)=O)=CN=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YS3375 Related Classifications
HY-189633 Related Classifications
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