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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).