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

In an in vitro study, an IL-3-independent Ba/F3 cell line expressing the KIT exon 9 A502_Y503dup primary activating mutation demonstrated reduced sensitivity to regorafenib (IC50: 138 nmol/L), imatini… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, a Ba/F3 cell line expressing KIT A502_Y503dup (502AY in the paper) mutation (overexpression) demonstrated sensitivity to sunitinib treatment (IC50: 5nM) similar to Ba/F3 cells ex… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

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 supp… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Ponatinib possesses potent activity against A829P KIT mutant cells in preclinical experiments. A preclinical study tested the effect of a tyrosine kinase inhibitor (TKI) on Ba/F3 cell lines with repre… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Several preclinical studies tested the effects of various tyrosine kinase inhibitors (TKIs) on Ba/F3 cell lines with representative primary sunitinib and imatinib sensitizing mutation del 557-558, whi… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Patient-derived GIST-T1/829 cells with driver mutation KIT 560-578 deletion and secondary KIT A829P mutations were tested for TKI responsiveness. 560-578del and A829P cells (Sunitinib IC50: 1168 nM an… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Several preclinical studies were done in order to test the effects of various tyrosine kinase inhibitors (TKIs) on KIT-mutant cell lines derived from Gastrointestinal Stromal Tumor (GIST) patients wit… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

A preclinical study was done in order to test the effects of a tyrosine kinase inhibitor (TKI) on the ponatinib-sensitive KIT-mutant cell line GIST-T1 derived from Gastrointestinal Stromal Tumor (GIST… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Ponatinib possesses potent activity against D816G KIT mutant in preclinical experiments.

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, a Ba/F3 cell line expressing KIT W557_K558del primary mutation (known to confer sensitivity to regorafenib) and KIT D816G secondary mutation, KIT D816G was associated with decrea… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Ponatinib possesses potent activity against D816H KIT mutant in preclinical experiments.

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, Ba/F3 cell lines expressing different KIT primary mutations (known to confer sensitivity to regorafenib) and KIT D816H secondary mutation, KIT D816H was associated with decreased… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, a Ba/F3 cell line expressing KIT 557-558del primary mutation (known to confer sensitivity to regorafenib) was incubated in various concentrations of ponatinib, sunitinib, or rego… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, Ba/F3 cell lines expressing KIT primary mutations and KIT D820A secondary mutation, KIT D820A was associated with similar sensitivity to ponatinib treatment compared to Ba/F3 cel… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, a Ba/F3 cell line expressing KIT W557_K558del primary mutation (known to confer sensitivity to regorafenib) and KIT D820A secondary mutation, KIT D820A was associated with decrea… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, an IL3 independent Ba/F3 cell line expressing KIT K550_W557del primary activating mutation demonstrated sensitivity to imatinib (IC50: 13nmol/L), sunitinib (IC50: 5nmol/L), regor… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, an IL3 independent Ba/F3 cell line expressing KIT K558NP primary activating mutation demonstrated sensitivity to imatinib (IC50: 2nmol/L), sunitinib (IC50: 2nmol/L ), regorafenib… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

The GIST882 patient derived cell line expressing KIT K642E mutation demonstrated sensitivity to ponatinib (IC50: 31nmol/L) and sunitinib (IC50: 54nmol/L) treatments. In comparison, the insensitve KIT-… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

A cell line derived from GIST882 patients expressing KIT K642E mutation demonstrated insensitivity to regorafenib (IC50: 503nmol/L) treatment. IC50 was determined by assessing cell viability.

PMID 25239608 · Garner et al., 2014 · Open in CIViC

A preclinical study tested the effect of a tyrosine kinase inhibitor (TKI) on Ba/F3 cell lines with primary ponatinib-sensitizing del 557-558 mutation, which induced IL-3 independent growth, and secon… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Ponatinib possesses potent activity against N882K KIT mutant in preclinical experiments.

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, an IL3 independent Ba/F3 cell line expressing KIT P551_E554delPMYE primary activating mutation demonstrated sensitivity to ponatinib treatment (IC50: 15nM). IC50 was determined b… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, an IL3 independent Ba/F3 cell line expressing KIT P551_E554delPMYE primary activating mutation demonstrated insensitivity to regorafenib (IC50: 141nmol/L), imatinib (IC50: 90nmol… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

A preclinical study tested the effects of a tyrosine kinase inhibitor (TKI) on Ba/F3 cell lines with representative primary imatinib-sensitizing mutation del 557-558, which induced IL-3 independent gr… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Several preclinical studies tested the effects of various tyrosine kinase inhibitors (TKIs) on Ba/F3 cell lines with representative primary ponatinib and sunitinib sensitizing mutation del 557-558, wh… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

A preclinical study tested the effects of a tyrosine kinase inhibitor (TKI) on Ba/F3 cell lines with representative primary regorafenib-sensitizing mutation del 557-558, which induced IL-3 independent… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Several preclinical studies tested the effects of various tyrosine kinase inhibitors (TKIs) on Ba/F3 cell lines with representative primary sunitinib-sensitizing mutation del 557-558 and secondary mut… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In 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

In 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

In an in vitro study, an IL3 independent Ba/F3 cell line expressing KIT V560D primary activating mutation demonstrated sensitivity to imatinib (IC50: 3nmol/L), sunitinib (IC50: 2nmol/L), regorafenib (… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro kinase study, a KIT V560G primary activating mutant kinase demonstrated sensitivity to imatinib (IC50: 38nmol/L vs. 640nmol/L), regorafenib (IC50: 27nmol/L vs. 533nmol/L), and ponatinib… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro kinase study, a KIT V560G primary activating mutant kinase demonstrated sensitivity to imatinib (IC50: 38nmol/L), regorafenib (IC50: 27nmol/L), and ponatinib (IC50: 0.3nmol/L) treatment… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro kinase study, a KIT V560G primary activating mutant kinase demonstrated sensitivity to sunitinib (IC50: 154nmol/L vs. 110nmol/L) treatments. It is assumed that the native KIT mutation i… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In the patient-derived cell line GIST430 harboring KIT V560_L576del primary activating mutation implanted in mice, imatinib and ponatinib were shown to reduce KIT phosphorylation compared to the vehic… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

A GIST430 patient derived cell line expressing KIT V560_L576del primary activating mutation demonstrated insensitivity to regorafenib (IC50: 191nmol/L) treatment. IC50 was determined by assessing cell… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, Ba/F3 cell lines expressing different KIT primary mutations (known to confer sensitivity to regorafenib) and KIT V654A secondary mutation, KIT V654A was associated with decreased… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, an IL3 independent Ba/F3 cell line expressing KIT W557_K558del primary activating mutation demonstrated sensitivity to imatinib (IC50: 27nmol/L) and ponatinib (IC50: 3nmol/L) tre… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, an IL3 independent Ba/F3 cell line expressing KIT W557_K558del primary activating mutation demonstrated sensitivity to sunitinib (IC50: 7 +/- 2nmol/L) and regorafenib (IC50: 30 … (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Ponatinib possesses potent activity against D820G KIT mutant in preclinical experiments.

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, a Ba/F3 cell line expressing KIT W557_K558del primary mutation (known to confer sensitivity to regorafenib) and KIT D820G secondary mutation, KIT D820G was associated with decrea… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In a set of preclinical experiments associated with gastrointestinal stromal tumor, the effects of the tyrosine kinase inhibitor regorafenib on Ba/F3 cell lines harboring the primary regorafenib-sensi… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

Several preclinical studies tested the effects of various tyrosine kinase inhibitors (TKIs) on Ba/F3 cell lines with primary TKI-sensitizing del 557-558 mutation, which induced IL-3 independent growth… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC

In an in vitro study, an IL3 independant Ba/F3 cell line expressing KIT V560D primary activating mutation demonstrated sensitivity to sunitinib treatment (IC50: 5nmol/L). IC50 was determined by assess… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC