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Table 1 Isogenic Ba/F3 model: apoptosis and proliferation assays - IC50s

From: Cell cycle-dependent activity of the novel dual PI3K-MTORC1/2 inhibitor NVP-BGT226 in acute leukemia

NVP-BEZ235   IC50 (nM) NVP-BGT226 IC50 (nM)
Induction of apoptosis   At 1000 nM (% apopt.) At 5000 nM (% apopt.) Induction of apoptosis   At 1000 nM (% apopt.) At 5000 nM (% apopt.)
Parental (w/ IL3) Not reached* 3 6 Parental (w/ IL3) 1821 7 99
KIT WT 1396 32 85 KIT WT 463 48 97
KIT D816V Not reached 4 23 KIT D816V 1791 7 99
KIT D816F 1244 40 87 KIT D816F 258 87 89
KIT D816Y 1363 5 73 KIT D816Y 118 89 96
FLT3 WT 8296 38 40 FLT3 WT 345 41 99
FLT3 S451F 741 49 70 FLT3 S451F 125 93 99
FLT3 ITD Not reached 19 27 FLT3 ITD 1079 38 98
FLT3 K663Q Not reached 17 16 FLT3 K663Q 1111 26 98
FLT3 D835V 458 52 86 FLT3 D835V 163 84 98
FLT3 D835Y Not reached 19 28 FLT3 D835Y 1073 33 98
FLT3 N841H Not reached 19 22 FLT3 N841H 1206 18 99
BCR/ABL1 Not reached 38 39 BCR/ABL1 262 56 97
Inhibition of proliferation   At 10 nM (% alive) At 100 nM (% alive) Inhibition of proliferation   At 10 nM (% alive) At 100 nM (% alive)
Parental (w/ IL3) 2398 89 98 Parental (w/IL3) 828 100 86
KIT WT 6 12 11 KIT WT 6 24 13
KIT D816V 8 40 38 KIT D816V 153 110 47
KIT D816Y 72 64 62 KIT D816Y 65 112 26
FLT3 WT 7 33 28 FLT3 WT 40 66 27
FLT3 K663Q 91 57 51 FLT3 K663Q 277 79 52
FLT3 ITD 7 13 4 FLT3 ITD 3 4 9
FLT3 D835V 10 50 51 FLT3 D835V 141 58 47
FLT3 D835Y 5 37 30 FLT3 D835Y 35 65 33
FLT3 N841H 9 43 47 FLT3 N841H 89 110 38
BCR/ABL1 131 58 50 BCR/ABL1 183 73 52
  1. *IC50s not reached (> 5 000 nM).