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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $38 | In Stock | |
5 mg | $88 | In Stock | |
10 mg | $143 | In Stock | |
25 mg | $295 | In Stock | |
50 mg | $513 | In Stock | |
100 mg | $818 | In Stock | |
1 mL x 10 mM (in DMSO) | $98 | In Stock |
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). |
Targets&IC50 | PLK4:0.26 nM(ki) |
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] |
Molecular Weight | 534.65 |
Formula | C33H34N4O3 |
Cas No. | 1338806-73-7 |
Smiles | O=C1[C@]2([C@@H](C2)C=3C=C4C(=CC3)C(/C=C/C5=CC=C(CN6C[C@@H](C)O[C@@H](C)C6)C=C5)=NN4)C=7C(N1)=CC=C(OC)C7 |
Relative Density. | 1.32 g/cm3 (Predicted) |
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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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