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Table 1 Inhibition of KIT kinases by HQP1351 at two different concentrations

From: Preclinical development of HQP1351, a multikinase inhibitor targeting a broad spectrum of mutant KIT kinases, for the treatment of imatinib-resistant gastrointestinal stromal tumors

KIT mutation

KIT exon

% of control

Inhibition rate (%)

10 nM

100 nM

10 nM

100 nM

KIT (wild-type)

–

2.8

0.05

97.2

99.95

KIT (L576P)

11

2.2

0

97.8

100

KIT (V559D)

11

1.4

0.05

98.6

99.95

KIT (A829P)

18

56

48

44

52

KIT (D816H)

17

58

28

42

72

KIT (D816 V)

17

83

21

17

79

KIT (V559D, T670I)

11/14

8.1

0.55

91.9

99.45

KIT (V559D, V654A)

11/13

56

6.2

44

93.8

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Cell & Bioscience

ISSN: 2045-3701

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