DcpS-IN-1
DcpS-IN-1 is an orally active DcpS inhibitor with an IC50 of 0.16 nM against hDcpS. DcpS-IN-1 exhibits anticancer activity against lung squamous cell carcinoma and head and neck squamous cell carcinoma. DcpS-IN-1 can be used in the research of solid tumors.
For research use only. We do not sell to patients.
- Formula: C20H19N7O2
- Molecular Weight:389.41
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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
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- References
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | EC50 |
33.8 nM
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Inhibition of FHIT-deficient NSCLC A549 cell viability incubated for 120 h by CellTiter-Glo Cell Viability Assay.
Inhibition of FHIT-deficient NSCLC A549 cell viability incubated for 120 h by CellTiter-Glo Cell Viability Assay.
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42593929 |
| EBC-1 | EC50 |
19 nM
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Inhibition of FHIT-deficient lung squamous cell carcinoma EBC-1 cell viability incubated for 120 h.
Inhibition of FHIT-deficient lung squamous cell carcinoma EBC-1 cell viability incubated for 120 h.
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42593929 |
| A253 cell line | EC50 |
17 nM
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Inhibition of FHIT-deficient head and neck squamous cell carcinoma A253 cell viability incubated for 120 h.
Inhibition of FHIT-deficient head and neck squamous cell carcinoma A253 cell viability incubated for 120 h.
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42593929 |
| HEK293 | IC50 |
4.4 μM
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Inhibition of hERG channel activity in hERG-overexpressing HEK-293 cells measured using a SyncroPatch 384i electrophysiology system with a standard 2-step voltage protocol.
Inhibition of hERG channel activity in hERG-overexpressing HEK-293 cells measured using a SyncroPatch 384i electrophysiology system with a standard 2-step voltage protocol.
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42593929 |
In Vitro
DcpS-IN-1 (Compound 17) (30 min) potently inhibits purified human DcpS protein with an IC50 of 0.16 nM[1].
DcpS-IN-1 exhibits excellent Caco-2 permeability with no efflux[1].
DcpS-IN-1 (0-10 μM; 120 h) inhibits FHIT-deficient NSCLC A549 cell viability with an EC50 of 33.8 nM and exhibits 203-fold selectivity over FHIT-overexpressing A549 cells[1].
DcpS-IN-1 (120 h) inhibits FHIT-deficient lung squamous cell carcinoma EBC-1 cell viability with an EC50 of 19 nM[1].
DcpS-IN-1 (120 h) inhibits FHIT-deficient head and neck squamous cell carcinoma A253 cell viability with an EC50 of 17 nM[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:FHIT-deficient NSCLC A549 cells
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Concentration:0-10 μM
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Incubation Time:120 h
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Result:Inhibited A549 cell viability with an EC50 of 33.8 nM.
Showed 203-fold selectivity relative to DcpS-insensitive FHIT-overexpressing A549 cells.
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Cell Line:FHIT-deficient lung squamous cell carcinoma EBC-1 cells
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Concentration:range of concentrations
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Incubation Time:120 h
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Result:Inhibited EBC-1 cell viability with an EC50 of 19 nM.
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Cell Line:FHIT-deficient head and neck squamous cell carcinoma A253 cells
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Concentration:range of concentrations
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Incubation Time:120 h
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Result:Inhibited A253 cell viability with an EC50 of 17 nM.
Parmacokinetics
| Species | Dose | Route | CLplasma | CLunbound | Vdss | T1/2 | Bioavailability |
|---|---|---|---|---|---|---|---|
| Mice[1] | 0.5 mg/kg | i.v. | 1.2 L/h/kg | 4.8 L/h/kg | 6 L/kg | 5.4 h | / |
| Mice[1] | 2.0 mg/kg | p.o. | / | / | / | / | 32 % |
| Rat[1] | 3.0 mg/kg | i.v. | 2.4 L/h/kg | 10 L/h/kg | 5.8 L/kg | 1.9 h | / |
| Rat[1] | 1.0 mg/kg | p.o. | / | / | / | / | 70 % |
| Dog[1] | 0.1 mg/kg | i.v. | 0.34 L/h/kg | 1.8 L/h/kg | 6.5 L/kg | 13.0 h | / |
| Monkey[1] | 0.1 mg/kg | i.v. | 0.77 L/h/kg | 9.6 L/h/kg | 1.8 L/kg | 1.7 h | / |
In Vivo
DcpS-IN-1 (1-5 mg/kg; p.o.; QD, BID; 25 days) exhibits dose-dependent tumor growth inhibition in A253 xenograft mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17-SCID (female, 7-9-week-old, EBC-1 lung squamous cancer xenograft via flank injection of 5×106 cells)[1]
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Dosage:2 mg/kg; 5 mg/kg; 1 mg/kg; 2.5 mg/kg
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Administration:p.o.; QD, BID; 25 days
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Result:Achieved tumor growth inhibition at 2 mg/kg QD.
Achieved tumor growth inhibition at 5 mg/kg QD.
Achieved tumor growth inhibition at 1 mg/kg BID.
Achieved tumor growth inhibition at 2.5 mg/kg BID.
Maintained healthy body weights throughout the study.
Chemical Information
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Molecular Weight 389.41
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Formula C20H19N7O2
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SMILES
CC(N=C1)=NC(C)=C1OC(N=C2)=CC=C2OCC3=CC=CC4=NC(N)=NC(N)=C43
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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)
DcpS-IN-1 Related Classifications
HY-189094 Related Classifications
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Keywords
- DcpS-IN-1
- DNA/RNA Synthesis
- FHIT-overexpressing A549 cells
- solid tumors
- DcpS
- FHIT-deficient head and neck squamous cell carcinoma A253 cell
- FHIT-deficient lung squamous cell carcinoma EBC-1 cell
- hERG
- solid tumor xenograft models
- FHIT-deficient NSCLC A549 cell
- cancer cells
- mRNA cap substrate
- Inhibitor
- inhibitor
- inhibit