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Table 2 Proliferation inhibitory effect of HQP1351 on GIST cells

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

Cell KIT genotype Sensitivity to imatinib IC50 (μM)
HQP1351 Ponatinib Sunitinib Regorafenib Imatinib
GIST T1 exon 11, 560–578 Sensitive 0.027 ± 0.021 0.021 ± 0.000 0.015 ± 0.012 0.079 ± 0.046 0.027 ± 0.005
GIST 430 exon 11, 560–576 Resistant 0.091 ± 0.021 0.134 ± 0.057 0.485 ± 0.168 3.321 ± 1.261 1.620 ± 0.318
exon13, V654A