Cimpuciclib tosylate 是一种选择性的 CDK4 抑制剂 (IC50: 0.49 nM)，具有抗肿瘤活性。
| Cas No. | 2408872-84-2 |
| 分子式 | C37H43FN8O4S |
| 分子量 | 714.85 |
| 溶解度 | DMSO : 200 mg/mL (279.78 mM; Need ultrasonic) |
| 储存条件 | 4°C, away from moisture |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Cimpuciclib tosylate is a selectiveCDK4inhibitor (IC50: 0.49 nM) that has anti-tumor activity[1]. 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 IC50value 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 |
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