APL-5125
APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer.
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- No. CAS: 2830619-57-1
- Fòrmula: C27H24F5N3O5
- Peso molecular:565.49
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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CK2α 0.348 nM (IC50) |
CK2α 0.095 nM (Ki) |
| Species | Dose | Route | Note | CL | Vdss | T1/2 | Tmax | F |
|---|---|---|---|---|---|---|---|---|
| Dog[1] | 3 mg/kg | i.v. | male | 2.8 mL/min/kg | 0.35 L/kg | 3.8 h | / | / |
| Mice[1] | 3 mg/kg | i.v. | female | 12.6 mL/min/kg | 0.32 L/kg | 1.6 h | / | / |
| Rat[1] | 3 mg/kg | i.v. | female | 5.1 mL/min/kg | 0.33 L/kg | 2.8 h | / | / |
| Rat[1] | 3 mg/kg | i.v. | male | 8.8 mL/min/kg | 0.44 L/kg | 2.3 h | / | / |
| Rat[1] | 3 mg/kg | p.o. | male;10% DMSO, 18% HP-β-cycladextrin,72% water (solution) | / | / | / | 0.25-1.0 h | 16.5 % |
| Rat[1] | 5 mg/kg | p.o. | female;10% DMSO, 18% HP-β-cycladextrin,72% water (solution) | / | / | / | 0.5-1.0 h | 36.1 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice bearing with HCT-116 cells[1]
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Dosage:10, 30 and 100 mg/kg
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Administration:Oral administration, once daily for 21 days
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Result:Showed tumor-growth inhibition with 45% at 100 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2830619-57-1
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Peso molecular 565.49
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Fòrmula C27H24F5N3O5
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SMILES
O=C(O)C1=CC2=NC(OCCOCCCCNCC3=CC(F)=C(OC(F)(F)F)C(F)=C3)=C4C=CN=CC4=C2C=C1
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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)
APL-5125 Related Classifications
HY-178980 Related Classifications
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