Cimpuciclib
Cimpuciclib is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity.
For research use only. We do not sell to patients.
- CAS No.: 2202767-78-8
- Formula: C30H35FN8O
- Molecular Weight:542.65
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
CDK4 0.49 nM (IC50) |
CDK6 9.56 nM (IC50) |
In Vitro
Cimpuciclib (example 63, 141.2 nM, 6 days) inhibits proliferation in colo205 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:Colo205 cells
-
Concentration:0-500 nM approximately
-
Incubation Time:6 days
-
Result:Inhibited cell proliferation with an IC50 value of 141.2 nM.
In Vivo
Cimpuciclib (5 mg/kg for rats, 50 mg/kg for colo205 tumor-bearing mice, oral administration) shows slow metabolic rate and maintains high concentration in the plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Colo205 tumor-bearing mice[1]
-
Dosage:50 mg/kg, twice a week
-
Administration:Oral gavage
-
Result:Inhibited tumor growth by 93.63%.
-
Animal Model:Rats, colo205 tumor-bearing mice[1]
-
Dosage:5 mg/kg for rats, 50 mg/kg for colo205 tumor-bearing mice.
-
Administration:Oral administration
-
Result:Pharmacokinetic profile of Cimpuciclib (example 63).
dose (mg/kg) Cmax (ng/mL) Tmax (h) AUC0-24 (ng/mL•h) t1/2 (h) 5 mg/kg (rats) 559.7 6 5414 2.4 50 mg/kg (mice) 7960 1 136782 14.8
Chemical Information
-
CAS No. 2202767-78-8
-
Molecular Weight 542.65
-
Formula C30H35FN8O
-
SMILES
O=C(N1CCC(CC1)NC2CC2)C3=CC=C(NC4=NC(C5=CC6=C(N=C(C)N6C(C)C)C=C5)=C(F)C=N4)N=C3C
-
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)