Ocifisertib(CFI-400945 free base)

SKU: orb1299868

Description

Ocifisertib (CFI-400945 free base) is an orally bioavailable, highly potent and selective PLK4 inhibitor with a Ki of 0.26 nM. This small molecule is a valuable research tool for studying centriole duplication and has demonstrated antitumor activity in both cellular assays and in vivo cancer models.

Research Area

Cell Biology, Immunology & Inflammation

Key Properties

• CAS Number: 1338806-73-7
• MW: 534.65
• Purity: 99.04% (May vary between batches)
• Formula: C₃₃H₃₄N₄O₃
• 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
• Target: Apoptosis,PLK
• Solubility: H2O:Insoluble;Ethanol:100 mg/mL (187.04 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.48 mM);DMSO:100 mg/mL (187.04 mM)

Bioactivity

• Target IC50:
  AURKB/INCENP:98 nM|TIE2/TEK:22 nM|TRKB:9 nM|AURKA:140 nM|PLK4:0.26 nM(Ki)|TRKA:6 nM
• 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).
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ocifisertib, PLK4, CFI 400945, CFI 400945 free base, CFI400945, CFI-400945, CFI400945 free base, CFI-400945 free base

Compound Identifiers

PubChem CID

58486178