| Identification | Back Directory | [Name]
Methanone, [4-(cyclopropylamino)-1-piperidinyl][6-[[5-fluoro-4-[2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinyl]amino]-2-methyl-3-pyridinyl]- | [CAS]
2202767-78-8 | [Synonyms]
Cimpuciclib
Methanone, [4-(cyclopropylamino)-1-piperidinyl][6-[[5-fluoro-4-[2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinyl]amino]-2-methyl-3-pyridinyl]- | [Molecular Formula]
C30H35FN8O | [MOL File]
2202767-78-8.mol | [Molecular Weight]
542.65 |
| Hazard Information | Back Directory | [Uses]
Cimpuciclib is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity[1]. | [in vivo]
Cimpuciclib (example 63, 50 mg/kg, oral gavage, twice a week) 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) 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 (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 |
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| [IC 50]
CDK4: 0.49 nM (IC50); CDK6: 9.56 nM (IC50) | [References]
[1] Liu Shiqiang, et al. Preparation of benzimidazole compound as kinase inhibitor. Patent WO 2018045956. |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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