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.
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- Formule: C20H19N7O2
- Masse moléculaire:389.41
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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.
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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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Masse moléculaire 389.41
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Formule 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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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)
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