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Table 1 Modulation of cytotoxicity of K562, HL60 and their variant resistant cells

From: Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML)

  DNR   Idarubicin   Mitox   HHT   Mylotarg  
  IC50 (μM) RMF IC50 (μM) RMF IC50 (μM) RMF IC50 (ng/ml) RMF IC50 (ng/ml) RMF
K562           
None 0.28 ± 0.09   0.071 ± 0.026   0.60 ± 0.21   57.3 ± 6.5    
Zosuquidar 0.26 ± 0.09 1.1 0.071 ± 0.042 1.0 0.095 ± 0.029 6.3 58.4 ± 10.1 1.0   
CsA 0.23 ± 0.12 1.2 0.068 ± 0.039 1.0 0.14 ± 0.05 4.3 56.6 ± 4.2 1.0   
K562/HHT40           
None 2.3 ± 0.2   0.27 ± 0.06   1.7 ± 0.2   197.6 ± 44.4    
Zosuquidar 0.66 ± 0.08 3.5 0.20 ± 0.07 1.4 0.33 ± 0.06 5.2 85.4 ± 2.9 2.3   
CsA 0.51 ± 0.08 4.5 0.24 ± 0.11 1.1 0.45 ± 0.06 3.8 91.3 ± 9.3 2.2   
K562/HHT90           
None 3.6 ± 1.5   0.17 ± 0.11   1.9 ± 0.9   409.6 ± 70.2    
Zosuquidar 0.37 ± 0.14 9.7 0.12 ± 0.09 1.4 0.13 ± 0.05 14.6 80.4 ± 8.3 5.8   
CsA 0.32 ± 0.19 11.3 0.10 ± 0.06 1.7 0.25 ± 0.18 7.6 81.8 ± 8.3 5.0   
K562/DOX           
None >50b   1.82 ± 0.17   >50   >720    
Zosuquidar 1.1 ± 0.4 >45.5 0.21 ± 0.03 8.7 0.53 ± 0.10 >94.3 88.8 ± 1.9 >8.1   
CsA 10.5 ± 1.6 >4.8 0.30 ± 0.10 6.1 4.29 ± 0.22 >11.7 639.1 ± 70.1 >1.1   
HL60           
None 0.16 ± 0.03   0.053 ± 0.004   0.48 ± 0.22   40.5 ± 5.2   131.9 ± 72.3  
Zosuquidar 0.13 ± 0.04 1.2 0.057 ± 0.008 0.9 0.09 ± 0.03 5.3 41.7 ± 3.1 1.0 83.8 ± 9.5 1.6
CsA 0.10 ± 0.02 1.6 0.033 ± 0.008 1.6 0.13 ± 0.07 3.7 33.6 ± 2.6 1.2 35.5 ± 1.0 3.7
HL60/ADR           
None 2.1 ± 0.4   0.51 ± 0.03   1.5 ± 0.2   60.7 ± 12.4   >2000  
Zosuquidar 2.4 ± 0.5 0.9 0.50 ± 0.03 1.0 1.4 ± 0.4 1.1 58.6 ± 4.6 1.0 >2000 ND
CsA 0.49 ± 0.04 4.3 0.30 ± 0.09 1.7 0.51 ± 0.03 2.9 48.7 ± 5.3 1.2 67.6 ± 7.6 >29.9
HL60/DNR           
None >40   0.51 ± 0.05   >20   489.9 ± 24.5   >2000  
Zosuquidar 0.49 ± 0.16 >81.6 0.14 ± 0.01 3.6 0.22 ± 0.06 >90.1 46.5 ± 9.7 10.5 620.5 ± 38.9 3.2
CsA 2.5 ± 0.8 >16 0.15 ± 0.00 3.4 1.4 ± 0.6 >14.3 60.3 ± 5.0 8.1 >2000 ND
  1. a. All values are the means determined in quadruplicate in three independent experiments.
  2. b. The maximal dose tested was 50 μM. IC50 was more than 50 μM, not determined.
  3. c. Zosuquidar = 0.3 μM, CsA = 2 μM.