| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (7.48 mM), Sonication is recommended.
Ethanol : 100 mg/mL (187.04 mM), Sonication is recommended.
H2O : Insoluble
DMSO : 100 mg/mL (187.04 mM), Heating to 50℃ is recommended.
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| Keywords | PLK4 | Ocifisertib | CFI-400945 free base | CFI400945 free base | CFI-400945 | CFI400945 | CFI 400945 free base | CFI 400945 |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
