CFI-400437 dihydrochloride

SKU: orb1218993

Description

CFI-400437 is a selective and potent polo-like kinase 4 (PLK4) inhibitor.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 1247000-76-5
• MW: 565.5
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₀Cl₂N₆O₂
• SMILES: CN1CCN(CC1)C2=NC=C(C=C2)/C=C/C3=C4C=CC(=CC5=C(NC6=C5C=C(C=C6)OC)O)C=C4N=N3.Cl.Cl
• Target: PLK
• Solubility: DMSO:5 mM

Bioactivity

• In Vivo:
  (1E)-CFI-400437 (25 mg/kg; intraperitoneal injection; daily for 21 days) dihydrochloride shows effective in a mouse xenograft model of tumor growth. The plasma levels of (1E)-CFI-400437 (50 mg/kg; IP; mice) dihydrochloride shows a Cmax of 92 ng/mL and AUC of 190 ng h/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i. e. , unbound compound in plasma is 1%. Animal model: 6-8 week old female CB-17 SCID mice (MDA-MB-468 mouse xenograft model). Dosage: 25 mg/kg. Administration: Intraperitoneal injection; daily for 21 days. Result: Effective in a mouse xenograft model of tumor growth. In this study, (1E)-CFI-400437 is weighed and suspended in PEG400: water (30: 70) and sonicated at rt for 30 min. The compound is dispensed in aliquots and stored at 20 C° for the duration of the study, and each aliquot was thawed at room temperature before each dose.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PLK