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

Table 2 Proliferation inhibitory effect of HQP1351 on GIST cells

Cell	KIT genotype	Sensitivity to imatinib	IC₅₀ (μM)
Cell	KIT genotype	Sensitivity to imatinib	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
GIST 430	exon13, V654A	Resistant	0.091 ± 0.021	0.134 ± 0.057	0.485 ± 0.168	3.321 ± 1.261	1.620 ± 0.318

ISSN: 2045-3701