Cimpuciclib tosylate

Cimpuciclib tosylate is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity[1].

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

CDK4:0.49 nM (IC50)

CDK6:9.56 nM (IC50)

Cimpuciclib (example 63, 141.2 nM, 6 days) tosylate inhibits proliferation of colo205 cells[1]. Cell Proliferation Assay[1] 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.

Cimpuciclib (example 63, 50 mg/kg, oral gavage, twice a week) tosylate inhibits tumor growth in colo205 tumor-bearing mice[1]. Cimpuciclib (5 mg/kg for rats, 50 mg/kg for colo205 tumor-bearing mice, oral administration) tosylate shows slow metabolic rate and maintains high concentration in the plasma[1]. 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 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

[1]. Liu Shiqiang, et al. Preparation of benzimidazole compound as kinase inhibitor. Patent WO 2018045956.