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.
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- 화학식: C23H22F3N4O4P
- 분자량:506.41
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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 (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.
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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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분자량 506.41
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YS3375 Related Classifications
HY-189633 Related Classifications
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