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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