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Table 1 Non-linear regression analysis of IC50s (Antiproliferation)

From: Quizartinib (AC220) is a potent second generation class III tyrosine kinase inhibitor that displays a distinct inhibition profile against mutant-FLT3, -PDGFRA and -KIT isoforms

Cell line Target IC50 (nM)
   Inhibition of proliferation
HMC1.1 KIT V560G 14
HMC1.2 KIT V560G/D816V 1727
HMC1.2, 0.5% FBS KIT V560G/D816V 263
p815 KIT D814Y (murine) 445
Kasumi-1 KIT N822K 36
M-07e + SCF KIT-activated 77
M-07e + GM-CSF GM-CSF signaling not reached*
EOL-1 FIP1L1-PDGFRA 1
K562 BCR/ABL not reached*
HL60 unknown not reached*
Jurkat unknown not reached*
MV4;11 FLT3 ITD (hemizygous) < 1
MOLM14 FLT3 ITD < 1
MOLM14 + DMSO FLT3 ITD not reached*
Pat.221 CBF AML (KIT WT) 675
Pat.279 CBF AML (KIT WT) / FLT3 amplification (subclone)? 3434
Pat.299 CBF AML (KIT WT) 7248
Pat.305 CBF AML (KIT WT) 7079
Pat.375 CBF AML (KIT N/A) 503
Pat.379 CBF AML (KIT WT) 806
Pat.368 FLT3 amplification ? 2700
Pat.601 FLT3 ITD 1153
Pat.176 FLT3 ITD (Beta1) not reached*
Pat.602 FLT3 ITD (Beta1) not reached*
  1. * tested up to 10 000 nM.
  2. The table summarizes estimated IC50 values obtained by non-linear regression analysis for the antiproliferative activity of quizartinib in leukemia cell lines and primary native leukemia blasts.
  3. The cell line HMC1.2 was additionally pre-treated with reduced serum (0.5% FBS) to address the influence of methodology aspects on sensitivity profiles. To exclude solvent-associated non-specific cytotoxicity, the MOLM-14 cell line was treated with DMSO using the highest concentration for the quizartinib dose experiments.