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Ref Type

Journal Article

PMID

(25239608)

Authors

Garner AP, Gozgit JM, Anjum R, Vodala S, Schrock A, Zhou T, Serrano C, Eilers G, Zhu M, Ketzer J, Wardwell S, Ning Y, Song Y, Kohlmann A, Wang F, Clackson T, Heinrich MC, Fletcher JA, Bauer S, Rivera VM

Title

Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients.

Journal	Vol	Issue	Date	Pages	Journal Short Title
Clinical cancer research : an official journal of the American Association for Cancer Research	20	22	2014 Nov 15	5745-5755	Clin Cancer Res

URL

Abstract Text

KIT is the major oncogenic driver of gastrointestinal stromal tumors (GIST). Imatinib, sunitinib, and regorafenib are approved therapies; however, efficacy is often limited by the acquisition of polyclonal secondary resistance mutations in KIT, with those located in the activation (A) loop (exons 17/18) being particularly problematic. Here, we explore the KIT-inhibitory activity of ponatinib in preclinical models and describe initial characterization of its activity in patients with GIST.The cellular and in vivo activities of ponatinib, imatinib, sunitinib, and regorafenib against mutant KIT were evaluated using an accelerated mutagenesis assay and a panel of engineered and GIST-derived cell lines. The ponatinib-KIT costructure was also determined. The clinical activity of ponatinib was examined in three patients with GIST previously treated with all three FDA-approved agents.In engineered and GIST-derived cell lines, ponatinib potently inhibited KIT exon 11 primary mutants and a range of secondary mutants, including those within the A-loop. Ponatinib also induced regression in engineered and GIST-derived tumor models containing these secondary mutations. In a mutagenesis screen, 40 nmol/L ponatinib was sufficient to suppress outgrowth of all secondary mutants except V654A, which was suppressed at 80 nmol/L. This inhibitory profile could be rationalized on the basis of structural analyses. Ponatinib (30 mg daily) displayed encouraging clinical activity in two of three patients with GIST.Ponatinib possesses potent activity against most major clinically relevant KIT mutants and has demonstrated preliminary evidence of activity in patients with refractory GIST. These data strongly support further evaluation of ponatinib in patients with GIST.

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Molecular Profile	Treatment Approach
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Gene Name	Source	Synonyms	Protein Domains	Gene Description	Gene Role
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Gene	Variant	Impact	Protein Effect	Variant Description	Associated with drug Resistance
KIT	W557_K558del	deletion	gain of function	KIT W557_K558del results in the deletion of 2 amino acids in the juxtamembrane domain (exon 11) of the Kit protein from amino acids 557 to 558 (PMID: 12918066). W557_K558del results in constitutive activation of Kit and increased Erk phosphorylation, and leads to increased invasiveness and expression of ETV1 in cell culture (PMID: 25239608, PMID: 26936919).
KIT	K558delinsNP	indel	unknown	KIT K558delinsNP results in a deletion of lysine (K) at amino acid 558 within the juxtamembrane domain (exon 11) of the Kit protein, combined with the insertion of an asparagine (N) and a proline (P) at the same location (PMID: 16226710). K558delinsNP has been identified in the scientific literature (PMID: 11526490, PMID: 25239608, PMID: 20651400), but has not been biochemically characterized and therefore, its effect on Kit protein function is unknown (PubMed, Nov 2024).
KIT	D816H	missense	gain of function	KIT D816H lies within the tyrosine kinase domain region 2 (exon 17) of the Kit protein (PMID: 19164557). D816H results in increased kinase activity, constitutive Kit phosphorylation, activation of Stat3 signaling, and transformation of cultured cells (PMID: 10362788, PMID: 11494148), and confers resistance to some Kit inhibitors (PMID: 25239608).	Y

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Showing 1 to 78 of 78 entries

Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
KIT M552_K558del	gastrointestinal stromal tumor	predicted - resistant	Ponatinib	Case Reports/Case Series	Actionable	In a clinical study, a GIST patient harboring KIT M552_K558del, resistant to multiple tyrosine kinase inhibitors, demonstrated resistance to Iclusig (ponatinib) treatment as indicated by disease progression after 4 weeks of treatment (PMID: 25239608).	25239608
KIT P551_W557delinsL	gastrointestinal stromal tumor	predicted - sensitive	Ponatinib	Case Reports/Case Series	Actionable	In a clinical study, a GIST patient harboring KIT P551_W557delinsL, resistant to Gleevec (imatinib), Sutent (sunitinib), and Stivarga (regorafenib), demonstrated sensitivity to Iclusig (ponatinib) treatment, which resulted in tumor regression and stable disease (PMID: 25239608).	25239608
KIT W557C KIT K558_V560del	gastrointestinal stromal tumor	predicted - sensitive	Ponatinib	Case Reports/Case Series	Actionable	In a clinical study, a GIST patient harboring KIT K558_V560del and KIT W557C, resistant to Gleevec (imatinib), Sutent (sunitinib), and Stivarga (regorafenib), demonstrated sensitivity when treated with Iclusig (ponatinib), which resulted in a radiologic response and stabilization for six months (PMID: 25239608).	25239608
KIT V560_L576del	gastrointestinal stromal tumor	sensitive	Ponatinib	Preclinical - Pdx & cell culture	Actionable	In a preclinical study, a patient derived GIST cell line harboring KIT V560_L576del demonstrated sensitivity to Iclusig (ponatinib) in both culture and PDX models, resulting in phosphorylation inhibition of Akt, Kit, and Erk (PMID: 25239608).	25239608
KIT V560_L576del	gastrointestinal stromal tumor	sensitive	Imatinib	Preclinical - Pdx & cell culture	Actionable	In a preclinical study, a patient derived GIST cell line harboring KIT V560_L576del demonstrated sensitivity to Gleevec (imatinib) in both culture and PDX models, resulting in phosphorylation inhibition of Akt, Kit, and Erk (PMID: 25239608).	25239608
KIT W557_K558del KIT Y823D	gastrointestinal stromal tumor	sensitive	Ponatinib	Preclinical - Pdx & cell culture	Actionable	In a preclinical study, a patient derived GIST cell line co-harboring KIT W557_K558del and KIT Y823D demonstrated sensitivity to Iclusig (ponatinib) in a PDX model, resulting in complete tumor regression (PMID: 25239608).	25239608
KIT W557_K558del	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells expressing KIT W557_K558del demonstrated sensitivity to treatment with Iclusig (ponatinib) in both culture and cell line xenograft models, resulting in reduced cell viability and near complete tumor regression (PMID: 25239608).	25239608
KIT W557_K558del KIT D816H	Advanced Solid Tumor	decreased response	Sunitinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816H demonstrated a decreased response to treatment with Sutent (sunitinib) in both culture and cell line xenograft models, resulting in only a slight decrease in tumor volume (PMID: 25239608).	25239608
KIT W557_K558del KIT D816H	Advanced Solid Tumor	decreased response	Imatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816H demonstrated a decreased response to treatment with Gleevec (imatinib) in both culture and xenograft models, resulting in only a slight decrease in tumor volume (PMID: 25239608).	25239608
KIT W557_K558del KIT D816H	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816H demonstrated sensitivity to treatment with Iclusig (ponatinib) in both culture and cell line xenograft models, resulting in reduced cell viability and tumor regression (PMID: 25239608).	25239608
KIT W557_K558del KIT T670I	Advanced Solid Tumor	sensitive	Sunitinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT T670I demonstrated sensitivity to treatment with Sutent (sunitinib) in both culture and cell line xenograft models, resulting in reduced cell viability, decreased tumor volume, and tumor regression (PMID: 25239608).	25239608
KIT W557_K558del KIT T670I	Advanced Solid Tumor	no benefit	Imatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT T670I demonstrated no response to treatment with Gleevec (imatinib) in both culture and xenograft models (PMID: 25239608).	25239608
KIT W557_K558del KIT V654A	Advanced Solid Tumor	sensitive	Sunitinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT V654A demonstrated sensitivity to treatment with Sutent (sunitinib) in both culture and cell line xenograft models, resulting in reduced cell viability, decreased tumor volume, and tumor regression (PMID: 25239608).	25239608
KIT W557_K558del KIT V654A	Advanced Solid Tumor	no benefit	Imatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT V654A demonstrated no response to treatment with Gleevec (imatinib) in both culture and xenograft models (PMID: 25239608).	25239608
KIT W557_K558del KIT V654A	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT V654A demonstrated sensitivity to treatment with Iclusig (ponatinib) in both culture and cell line xenograft models, resulting in reduced cell viability and decreased tumor volume (PMID: 25239608).	25239608
KIT V560_Y578del	gastrointestinal stromal tumor	sensitive	Ponatinib	Preclinical - Patient cell culture	Actionable	In a preclinical study, a patient-derived gastrointestinal stromal tumor (GIST) cell line harboring KIT V560_Y578del demonstrated sensitivity to Iclusig (ponatinib) in culture (PMID: 25239608).	25239608
KIT V560_Y578del KIT T670I	gastrointestinal stromal tumor	sensitive	Sunitinib	Preclinical - Cell culture	Actionable	In a preclinical study, a patient-derived gastrointestinal stromal tumor (GIST) cell line co-harboring KIT V560_Y578del and KIT T670I demonstrated sensitivity to treatment with Sutent (sunitinib) (PMID: 25239608).	25239608
KIT W557_K558del KIT A829P	Advanced Solid Tumor	resistant	Sunitinib	Preclinical - Biochemical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT A829P were resistant to Sutent (sunitinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT A829P	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, cells expressing KIT A829P demonstrated sensitivity to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT D816H	Advanced Solid Tumor	resistant	Regorafenib	Preclinical	Actionable	In a preclinical study, KIT D816H demonstrated resistance to Stivarga (regorafenib) in an in vitro assay, and conferred secondary resistance to Stivarga (regorafenib) in transformed cells expressing other KIT mutations (PMID: 25239608).	25239608
KIT D816H	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, cells expressing KIT D816H demonstrated sensitivity to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT D820E	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, cells expressing KIT D820E demonstrated sensitivity to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT exon9	Advanced Solid Tumor	resistant	Imatinib	Preclinical	Actionable	In a preclinical study, Gleevec (imatinib) had no effect on transformed cells expressing a KIT exon 9 mutation in culture (PMID: 25239608).	25239608
KIT exon9	Advanced Solid Tumor	resistant	Regorafenib	Preclinical	Actionable	In a preclinical study, Stivarga (regorafineb) had no effect on transformed cells expressing a KIT exon 9 mutation in culture (PMID: 25239608).	25239608
KIT exon9	Advanced Solid Tumor	sensitive	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing a KIT exon 9 mutation demonstrated sensitivity to treatment with Sutent (sunitinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT exon9	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing a KIT exon 9 mutation demonstrated sensitivity to treatment with Iclusig (ponatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT K558delinsNP	Advanced Solid Tumor	sensitive	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT K558delinsNP demonstrated sensitivity to treatment with Gleevec (imatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT K558delinsNP	Advanced Solid Tumor	sensitive	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT K558delinsNP demonstrated sensitivity to treatment with Sutent (sunitinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT K558delinsNP	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT K558delinsNP demonstrated sensitivity to treatment with Iclusig (ponatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT K558delinsNP	Advanced Solid Tumor	sensitive	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT K558delinsNP demonstrated sensitivity to treatment with Stivarga (regorafenib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT K642E	gastrointestinal stromal tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, a patient derived GIST cell line harboring KIT K642E demonstrated sensitivity to Iclusig (ponatinib) in culture (PMID: 25239608).	25239608
KIT P551_E554del	Advanced Solid Tumor	resistant	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT P551_E554del were resistant to treatment with Gleevec (imatinib) in culture (PMID: 25239608).	25239608
KIT P551_E554del	Advanced Solid Tumor	resistant	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT P551_E554del were resistant to treatment with Stivarga (regorafenib) in culture (PMID: 25239608).	25239608
KIT P551_E554del	Advanced Solid Tumor	resistant	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT P551_E554del were resistant to treatment with Sutent (sunitinib) in culture (PMID: 25239608).	25239608
KIT P551_E554del	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT P551_E554del demonstrated sensitivity to treatment with Iclusig (ponatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT P551_K558del	Advanced Solid Tumor	sensitive	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT P551_K558del (reported as K550_W557del) demonstrated sensitivity to treatment with Stivarga (regorafenib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT P551_K558del	Advanced Solid Tumor	sensitive	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT P551_K558del (reported as K550_W557del) demonstrated sensitivity to treatment with Gleevec (imatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT P551_K558del	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT P551_K558del (reported as K550_W557del) demonstrated sensitivity to treatment with Iclusig (ponatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT P551_K558del	Advanced Solid Tumor	sensitive	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT P551_K558del (reported as K550_W557del) demonstrated sensitivity to treatment with Sutent (sunitinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT T670I	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, cells expressing KIT T670I demonstrated sensitivity to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT V559D	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, cells expressing KIT V559D demonstrated sensitivity to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT V560_L576del KIT V654A	gastrointestinal stromal tumor	sensitive	Sunitinib	Preclinical	Actionable	In a preclinical study, a patient derived GIST cell line co-harboring KIT V560_L576del and KIT V654A demonstrated sensitivity to treatment with Sutent (sunitinib) (PMID: 25239608).	25239608
KIT V560_Y578del	gastrointestinal stromal tumor	sensitive	Imatinib	Preclinical	Actionable	In a preclinical study, a patient derived GIST cell line harboring KIT V560_Y578del demonstrated sensitivity to Gleevec (imatinib) in culture (PMID: 25239608).	25239608
KIT V560_Y578del KIT A829P	gastrointestinal stromal tumor	decreased response	Sunitinib	Preclinical	Actionable	In a preclinical study, a patient derived GIST cell line co-harboring KIT V560_Y578del and KIT A829P demonstrated a decreased response to treatment with Sutent (sunitinib) (PMID: 25239608).	25239608
KIT V560_Y578del KIT D816E	gastrointestinal stromal tumor	decreased response	Sunitinib	Preclinical	Actionable	In a preclinical study, a patient derived GIST cell line co-harboring KIT V560_Y578del and KIT D816E demonstrated a decreased response to treatment with Sutent (sunitinib) (PMID: 25239608).	25239608
KIT V560_Y578del KIT T670I	gastrointestinal stromal tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, a patient derived GIST cell line co-harboring KIT V560_Y578del and KIT T670I demonstrated sensitivity to treatment with Iclusig (ponatinib) (PMID: 25239608).	25239608
KIT V560D	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT V560D demonstrated sensitivity to treatment with Iclusig (ponatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT V560D	Advanced Solid Tumor	sensitive	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT V560D demonstrated sensitivity to treatment with Stivarga (regorafineb) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT V560D	Advanced Solid Tumor	sensitive	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT V560D demonstrated sensitivity to treatment with Gleevec (imatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT V560D	Advanced Solid Tumor	sensitive	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT V560D demonstrated sensitivity to treatment with Sutent (sunitinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT V560G	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, cells expressing KIT V560G demonstrated sensitivity to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT V654A	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, cells expressing KIT V654A demonstrated some sensitivity to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del	Advanced Solid Tumor	sensitive	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT W557_K558del demonstrated sensitivity to treatment with Stivarga (regorafineb) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT W557_K558del	Advanced Solid Tumor	sensitive	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT W557_K558del demonstrated sensitivity to treatment with Sutent (sunitinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT W557_K558del	Advanced Solid Tumor	sensitive	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells expressing KIT W557_K558del demonstrated sensitivity to treatment with Gleevec (imatinib) in culture, resulting in reduced cell viability (PMID: 25239608).	25239608
KIT W557_K558del KIT A829P	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT A829P were sensitive to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT A829P	Advanced Solid Tumor	resistant	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT A829P were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT A829P	Advanced Solid Tumor	conflicting	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT A829P were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D816G	Advanced Solid Tumor	resistant	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816G were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D816G	Advanced Solid Tumor	resistant	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816G were resistant to Sutent (sunitinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D816G	Advanced Solid Tumor	resistant	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816G were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D816G	Advanced Solid Tumor	resistant	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816G were sensitive to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D816H	Advanced Solid Tumor	decreased response	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816H demonstrated a decreased response to treatment with Stivarga (regorafenib) in culture (PMID: 25239608).	25239608
KIT W557_K558del KIT D820A	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820A were sensitive to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D820A	Advanced Solid Tumor	conflicting	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820A were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D820A	Advanced Solid Tumor	resistant	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820A were resistant to Sutent (sunitinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D820A	Advanced Solid Tumor	resistant	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820A were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D820G	Advanced Solid Tumor	resistant	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820G were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D820G	Advanced Solid Tumor	resistant	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820G were resistant to Sutent (sunitinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D820G	Advanced Solid Tumor	resistant	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820G were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT D820G	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820G were sensitive to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT N822K	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT N822K were sensitive to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT N822K	Advanced Solid Tumor	conflicting	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT N822K were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT N822K	Advanced Solid Tumor	resistant	Imatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT N822K were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT N822K	Advanced Solid Tumor	resistant	Sunitinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT N822K were resistant to Sutent (sunitinb) in an in vitro kinase assay (PMID: 25239608).	25239608
KIT W557_K558del KIT T670I	Advanced Solid Tumor	sensitive	Ponatinib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT T670I demonstrated sensitivity to treatment with Iclusig (ponatinib) in both culture and cell line xenograft models, resulting in reduced cell viability and decreased tumor volume (PMID: 25239608).	25239608
KIT W557_K558del KIT T670I	Advanced Solid Tumor	decreased response	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT T670I demonstrated a decreased response to treatment with Stivarga (regorafenib) compared to cells expressing KIT W557_K558del alone in culture (PMID: 25239608).	25239608
KIT W557_K558del KIT V654A	Advanced Solid Tumor	resistant	Regorafenib	Preclinical	Actionable	In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT V654A demonstrated resistance to treatment with Stivarga (regorafenib) in culture (PMID: 25239608).	25239608

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