| KIT V559D11 |
|---|
| CHMFL-KIT-031 | Gastrointestinal Stromal Tumor | Predictive | D | Supports Sensitivity Response | 3 | submitted | EID7870A novel compound identified in a high-throughput screen is highly selective for KIT V559D in cell lines and mice models. In mice, there was a dose-dependent reduction in tumor size. PMID 29340041 · Yu et al., 2017 · Open in CIViC | civic |
| Dasatinib | Melanoma | Predictive | D | Supports Sensitivity Response | — | submitted | EID4107In an in vitro study, Ba/F3 cells expressing KIT V559D mutation were found to have increased sensitivity to dasatinib (IC50: 22 nM). Sensitivity was determined by assessing cell proliferation, apopto… (full text at CIViC) PMID 17372901 · Antonescu et al., 2007 · Open in CIViC | civic |
| 〃 | Solid NeoplasmCURATED_BROADER | Predictive | D | Supports Sensitivity Response | — | rejected | EID4114In an in vitro study of gastrointestinal tumors, HEK-293 cells expressing KIT V559D mutation were found to have sensitivity to dasatinib treatment. (IC50: 8nM). Sensitivity was determined by assessin… (full text at CIViC) PMID 16046538 · Carter et al., 2005 · Open in CIViC | civic |
| Dasatinib + Imatinib + Nilotinib + SorafenibSubstitutes | Gastrointestinal Stromal Tumor | Predictive | D | Supports Sensitivity Response | 4 | submitted | EID3033dasatinib inhibited cell growth of imatinib-sensitive KIT V559D with an IC50 of 27 nmol/L, whereas imatinib, nilotinib, and sorafenib had an IC50 of 63, 44, and 66 nmol/L, respectively. PMID 17699867 · Guo et al., 2007 · Open in CIViC | civic |
| Imatinib | Gastrointestinal Stromal Tumor | Predictive | C | Supports Sensitivity Response | 3 | accepted | EID3028A patient with an uncontrolled relapse of c-kit-positive mesenchymal tumor in descending part of the duodenum had received 400mg Imatinib daily for more than 10 years at the time of publication. He re… (full text at CIViC) PMID 22114577 · Cameron et al., 2011 · Open in CIViC | civic |
| Dasatinib + Imatinib + PD-180970 + Sunitinib + TandutinibSubstitutes | Malignant NeoplasmALIAS | Predictive | D | Supports Sensitivity Response | 2 | accepted | EID3029KIT(V559D) were expressed in HEK-293 cells (in vitro). Imatinib, BMS-354825 (dasatinib), PD-180970, MLN-518 (tandutinib), and SU-11248 bind variant V559D with high affinity (Kd =< 20 nM), and inhibit … (full text at CIViC) PMID 16046538 · Carter et al., 2005 · Open in CIViC | civic |
| Imatinib + Ponatinib + RegorafenibSubstitutes | Gastrointestinal Stromal Tumor | Predictive | D | Supports Sensitivity Response | 2 | accepted | EID4459In an in vitro kinase study, a KIT V559D primary activating mutant kinase demonstrated sensitivity to imatinib (IC50: 36nmol/L vs. 640nmol/L), regorafenib (IC50: 57nmol/L vs. 533nmol/L), and ponatinib… (full text at CIViC) PMID 25239608 · Garner et al., 2014 · Open in CIViC | civic |
| Sunitinib | Gastrointestinal Stromal Tumor | Predictive | C | Supports Resistance | — | submitted | EID4108In a phase 1/2 trial of 97 gastrointestinal stromal tumor patients, patients with KIT exon 11 mutations (44/77) treated with sunitinib were associated with shorter progression free survival (5.1mo vs.… (full text at CIViC) PMID 18955458 · Heinrich et al., 2008 · Open in CIViC | civic |
| 〃 | Gastrointestinal Stromal Tumor | Predictive | C | Supports Resistance | — | submitted | EID4110In a retrospective study of 1124 sunitinib-treated gastrointestinal stromal tumor patients, patients with primary KIT exon 11 mutations (n=143) were associated with decreased progression free surviva… (full text at CIViC) PMID 26772734 · Reichardt et al., 2016 · Open in CIViC | civic |
| 〃 | Gastrointestinal Stromal Tumor | Predictive | D | Supports Resistance | — | submitted | EID4109In an in vitro study, a 32D cell line expressing KIT V559D mutation (overexpression) demonstrated increased sensitivity to sunitinib treatment (IC50: 2.0nM) compared to 32D cells expressing wild-type … (full text at CIViC) PMID 24205792 · Zhao et al., 2014 · Open in CIViC | civic |
| 〃 | Gastrointestinal Stromal Tumor | Predictive | D | Supports Resistance | — | submitted | EID4592In an in vitro study, a Ba/F3 cell line expressing KIT K558NP mutation (overexpression) demonstrated improved sensitivity to sunitinib treatment (IC50: 2nM vs. 8nM) compared to Ba/F3 cells expressing … (full text at CIViC) PMID 25239608 · Garner et al., 2014 · Open in CIViC | civic |