Novel FLT3/AURK multikinase inhibitor is efficacious against sorafenib-refractory and sorafenib-resistant hepatocellular carcinoma

Table 1 Antiproliferative activity of DBPR114 in human HCC cell lines in vitro

Cell line	Histopathology	Growth inhibition, IC₅₀ (μM)
Cell line	Histopathology	DBPR114	Sorafenib
HA22T/VGH	HCC, p53^MT, poorly differentiated, HBV⁺/HCV⁻	0.7	8.6
HA59T/VGH	HCC, p53^MT, poorly differentiated, HBV⁺/HCV⁻	1.7	8.3
Huh1	HCC, p53^MT, moderately differentiated, HBV⁻/HCV⁻	1.9	9.5
Huh7	HCC, p53^MT, moderately differentiated, HBV⁻/HCV⁻	1.7	8.4
PLC/PRF/5	HCC, p53^MT, moderately differentiated, HBV⁺/HCV⁻	2.1	6.5
Hep3B	HCC, p53^null, well differentiated, HBV⁺/HCV⁻	1.5	6.6

HCC cells were treated with DBPR114 or sorafenib at various concentrations for 72 h. Cell viability was assessed through WST-8 cell proliferation assay. IC₅₀ values represent the mean of two independent experiments with eight concentrations and six replicates per concentration
p53^null: p53 Deletion; p53^MT : Mutant-type p53; HBV⁺ : Hepatitis B-positive virus; HBV⁻: Hepatitis B-negative virus; HCV⁻^-: Hepatitis C-negative virus

ISSN: 1423-0127