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.
For research use only. We do not sell to patients.
- CAS No.: 2830619-57-1
- Formula: C27H24F5N3O5
- Molecular Weight:565.49
-
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]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CK2α 0.348 nM (IC50) |
CK2α 0.095 nM (Ki) |
Parmacokinetics
| 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 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mice bearing with HCT-116 cells[1]
-
Dosage:10, 30 and 100 mg/kg
-
Administration:Oral administration, once daily for 21 days
-
Result:Showed tumor-growth inhibition with 45% at 100 mg/kg.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2830619-57-1
-
Molecular Weight 565.49
-
Formula C27H24F5N3O5
-
SMILES
O=C(O)C1=CC2=NC(OCCOCCCCNCC3=CC(F)=C(OC(F)(F)F)C(F)=C3)=C4C=CN=CC4=C2C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
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.
-
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
APL-5125 Related Classifications
HY-178980 Related Classifications
Powered by Bioz