Cimpuciclib 是一种选择性的CDK4抑制剂 (IC50: 0.49 nM)，具有抗肿瘤活性。
| 生物活性 | Cimpuciclib is a selectiveCDK4inhibitor (IC50: 0.49 nM) that has anti-tumor activity[1]. |
| IC50& Target[1] | CDK4 0.49 nM (IC50) | CDK6 9.56 nM (IC50) |
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体外研究
(In Vitro) | Cimpuciclib (example 63, 141.2 nM, 6 days) inhibits proliferation in 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 IC50value of 141.2 nM. |
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体内研究
(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/mLoh) | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
