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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.