Malignant Bone Marrow Neoplasm

AML MOLM14 cells were cocultured with FLT3 inhibitor AC220 (10 nM) and selected proteins expressed in the bone marrow microenvironment. FL and FGF2 were the only proteins that increased viability >2 s… (full text at CIViC)

PMID 27671675 · Traer et al., 2016 · Open in CIViC

In this preclinial trial, the AML cell line KG1 with FGFR1OP2-FGFR1 mutation was treated with Ponatinib. This drug effectively inhibits both FGFR phosphorylation and viability for KG1 cells at IC50 va… (full text at CIViC)

PMID 21482694 · Gozgit et al., 2011 · Open in CIViC

In an in vitro kinase study, the recombinant FGFR1 V561M mutant kinase demonstrated resistance to bosutinib treatment at concentrations of 1μM and 10μM (activity %: 87 and 41) when compared to wild ty… (full text at CIViC)

PMID 19039322 · Remsing Rix et al., 2009 · Open in CIViC

In an in vitro kinase study, the recombinant FGFR1 V561M mutant kinase demonstrated resistance to dasatinib treatment at concentrations of 1μM and 10μM (activity %: 100 and 64) when compared to wild t… (full text at CIViC)

PMID 19039322 · Remsing Rix et al., 2009 · Open in CIViC

In an in vitro kinase study, the recombinant FGFR2 N549H mutant kinase demonstrated sensitivity to bosutinib treatment at concentrations of 1μM and 10μM (activity %: 32 and 3) when compared to wild ty… (full text at CIViC)

PMID 19039322 · Remsing Rix et al., 2009 · Open in CIViC

In an in vitro kinase study, the recombinant FGFR2 N549H mutant kinase demonstrated sensitivity to dasatinib treatment at concentrations of 1μM and 10μM (activity %: 6 and -1) when compared to wild ty… (full text at CIViC)

PMID 19039322 · Remsing Rix et al., 2009 · Open in CIViC

In this phase II, open-label, non-randomized trial, 36 patients with the myeloproliferative neoplasms chronic eosinophilic leukemia, CEL (n = 23) and hypereosinophilic syndrome, HES (n = 13) were enro… (full text at CIViC)

PMID 18950453 · Metzgeroth et al., 2008 · Open in CIViC

In this preclinial trial, the AML cell line EOL1 with FIP1L1-PDGFR alpha mutation was treated with Ponatinib. This drug effectively inhibits both PDGFR phosphorylation and viability for EOL1 cells at … (full text at CIViC)

PMID 21482694 · Gozgit et al., 2011 · Open in CIViC

A panel of 13 FLT3 tyrosine kinase inhibitors was tested against Ba/F3 cells transfected with FLT3 D593del using MTT growth/survival assay, and results were compared to Ba/F3 cells transfected with FL… (full text at CIViC)

PMID 28077790 · Nguyen et al., 2017 · Open in CIViC

A panel of 13 FLT3 tyrosine kinase inhibitors was tested against Ba/F3 cells transfected with FLT3 D593del using MTT growth/survival assay, and results were compared to Ba/F3 cells transfected with FL…

In a study of 82 newly diagnosed myelodysplastic syndrome (MDS) patients followed through to progression to acute myeloid leukemia (AML) (n =70), the incidence of FLT3 (ITD, TKD) and NRAS mutations at… (full text at CIViC)

PMID 14737077 · Shih et al., 2004 · Open in CIViC

In a Phase 1-2 trial of patients with relapsed / refractory AML, patients were enrolled in 7 dose-escalation or dose-expansion cohorts. Gilteritinib monotherapy was well tolerated, generated high resp… (full text at CIViC)

PMID 28645776 · Perl et al., 2017 · Open in CIViC

In a retrospective study of 15 acute myeloid leukemia patients, the patients with FLT3 D835 mutation (n=2) were associated with improved response to sunitinib treatment (2/2 vs. 2/7) compared to FLT3 … (full text at CIViC)

PMID 15459012 · Fiedler et al., 2005 · Open in CIViC

D835G was originally identified from an AML patient. Transfection of D835G into Ba/F3 cells led to IL3 independent growth, indicating an oncogenic driver effect for the variant in these cells. This ev… (full text at CIViC)

PMID 28077790 · Nguyen et al., 2017 · Open in CIViC

Ba/F3 cells were transfected to express FLT3-ITD or FLT3 tyrosine kinase domain mutations. Immunoblots revealed gilteritinib IC50s of 2nM, 1.6nM, and 5nM for D835H, FLT3-ITD, and wildtype (cell line: … (full text at CIViC)

PMID 27908881 · Lee et al., 2017 · Open in CIViC

Three children with relapsed or refractory FLT3-ITD-positive AML were treated with sorafenib. FLT3 mutations were assessed before treatment and at the time of resistance. During the initiation of the … (full text at CIViC)

PMID 23969938 · Baker et al., 2013 · Open in CIViC

Mouse Ba/F3 cells with FLT3 mutations were evaluated for sorafenib resistance. Cells with single FLT3 (D835H/Y) mutants were resistant to sorafenib (IC50 81 nm/210 nM) whereas cells with FLT3 (ITD) m… (full text at CIViC)

PMID 23969938 · Baker et al., 2013 · Open in CIViC

A 62-year-old female patient (AML5) was refractory to conventional chemotherapy and developed disease progression to quizartinib due to a D835I mutation. Using MTT to measure cytotoxicity, gilteritini… (full text at CIViC)

PMID 27908881 · Lee et al., 2017 · Open in CIViC

In this study, records of 69 FLT3 mutated AML patients treated with different FLT3 inhibitors were analyzed for emergence of new mutations. Before the start of therapy with a FLT3 inhibitor, 60 (87%) … (full text at CIViC)

PMID 24737502 · Alvarado et al., 2014 · Open in CIViC

D835N was originally identified from an AML patient. Transfection of D835N into Ba/F3 cells led to IL3 independent growth, indicating an oncogenic driver effect for the variant in these cells. This ev… (full text at CIViC)

PMID 28077790 · Nguyen et al., 2017 · Open in CIViC

In a phase 3 trial comparing gilteritinib (120 mg/day) to salvage chemotherapy (SC) in adults with relapsed or refractory FLT3- mutated AML, patients were required to have FLT3 ITD or TKD (tyrosine ki… (full text at CIViC)

PMID 31665578 · Perl et al., 2019 · Open in CIViC

429 AML, 29 MDS, 36 ALL, 14 adult T-Cell leukemia, 17 malignant lymphoma, 10 CLL, 40 multiple myeloma, 11 CML and 3 essential thrombocytosis patients were analyzed for FLT3 gen mutation and FLT3 D835… (full text at CIViC)

PMID 11290608 · Yamamoto et al., 2001 · Open in CIViC

The study is conducted with 144 AML patients. 6 of the normal karyotype patients with AML(n = 51), have FLT3 mutation. 2 of these mutations have been reported as D835V mutations.(%33 among FLT3 mutati… (full text at CIViC)

PMID 26297285 · El Halabi et al., 2015 · Open in CIViC

Cos7 cells transfected with mutant FLT3 D835Y cDNA demonstrated FLT3 ligand-independent tyrosine phosphorylation. 32D cells stably expressing mutant FLT3 D835Y proliferated without either IL-3 or reco… (full text at CIViC)

PMID 11290608 · Yamamoto et al., 2001 · Open in CIViC

Ba/F3 cells expressing FLT3 D835Y were stably transfected, cultured for 48 hours and then cell viability was analyzed. Wild-type FLT3 cells grown with IL-3 or in the absence of IL-3 served as positive… (full text at CIViC)

PMID 29372308 · Marhäll et al., 2018 · Open in CIViC