Name | Ocifisertib(CFI-400945 free base) |
Description | Ocifisertib (CFI-400945 free base) is a potent, selective and orally active inhibitor of polo-like kinase 4 (PLK4; Ki value 0.26 nM; IC50 value 2.8 nM). |
In vitro | METHODS: HCT116 cells with FLAG-tagged full-length PLK4 were treated with Ocifisertib (CFI-400945 free base) for 4 hours, and the lysates were analyzed by immunoblotting.
RESULTS In cells overexpressing PLK4, Ocifisertib inhibited PLK4 autophosphorylation at serine 305 with an EC50 value of 12.3 nM.[1] |
In vivo | METHODS: PK analysis was performed in mice treated with ocifisertib (CFI-400945 free base) (3.75-104 mg/kg, oral).
RESULTS CFI-400945 was rapidly absorbed after oral administration, reaching maximum plasma concentrations (Cmax) of 0.25–11.68 μg/mL; the elimination half-life was 3.7-4.2 hours at 3.75-26 mg/kg, but was prolonged with increasing doses (5.4 and 6.9 hours at 52 and 104 mg/kg, respectively). [1] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | Ethanol : 100 mg/mL (187.04 mM) H2O : Insoluble DMSO : 100 mg/mL (187.04 mM), Heating to 50℃ is recommended.
|
Keywords | CFI400945 free base | CFI-400945 | Ocifisertib | CFI-400945 free base | CFI 400945 free base | CFI400945 | CFI 400945 |
Inhibitors Related | Onvansertib | Plogosertib | T521 | (E/Z)-Rigosertib sodium | SBE13 Hydrochloride | Pyridoxine | Rigosertib sodium | 3MB-PP1 | Ro3280 | Poloxin-2 | BI 2536 | GSK461364 |
Related Compound Libraries | 经典已知活性库 | 激酶抑制剂库 | 药物功能重定位化合物库 | 抑制剂库 | 口服活性化合物库 | 临床期小分子药物库 | 已知活性化合物库 | 细胞周期化合物库 | 抗癌化合物库 | 抗癌活性化合物库 |