1616420-30-4

CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.

PLK4: 2.8 nM (IC₅₀); AURKA: 140 nM (IC₅₀); AURKB/INCENP: 98 nM (IC₅₀); TIE2/TEK: 22 nM (IC₅₀); TRKA: 6 nM (IC₅₀); TRKB: 9 nM (IC₅₀)

[1] Sampson PB, 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 8;58(1):147-69. PMID:25723005
[2] Mason JM, et al. Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent. Cancer Cell. 2014 Aug 11;26(2):163-76. DOI:10.1016/j.ccr.2014.05.006