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Background Information:
CFI-400945 is an orally bioavailable, clinical stage and ATP-competitive inhibitor of PLK4 (Polo-like kinase 4). Enantiomerically pure CFI-400945 (1R, 2S – enantiomer) potently inhibits the activity of PLK4, with a Ki value of 0.2 nM (enzymatic assay), and EC50 value of 12 nM (measuring inhibition of PLK4 autophosphorylation in cell overexpressing PLK4) (Ref. 2), and highly selective against PLK1, 2, 3 (no significant inhibition at 50 µM) (ref. 2). Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death (Ref 1). Oral administration of CFI-400945 to mice bearing human cancer xenografts results in the significant inhibition of tumor growth at doses that are well tolerated. Increased antitumor activity in vivo was observed in PTEN-deficient compared to PTEN wild-type cancer xenografts (Ref 1).
Reference:
1. J. M. Mason, et al, Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent. Cancer Cell. 2014, 26(2):163-76.
2. P. B. Sampson, et al, The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl)-1H-indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent. J Med Chem, 2015 Jan; 58(1):147-69.
APIM050030: CFI-400945
CAS No.: 1338806-73-7.
Molecular Formula: C33H34N4O3.
Molecular Weight: 534.7 (or refer to Certificate of Analysis, batch specific).
Purity: >99.5% chem and optical purity (by achiral and chiral HPLCs).
QC: HPLC-MS, 1H-NMR, Chiral HPLC and quantitative elemental analysis.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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