Leukemia

In a preclinical trial, multiple experiments testing the effectiveness of ponatinib on the mutation FLT3-ITD in acute myeloid leukemia (AML) were conducted. Ponatinib was very effective in targeting t… (full text at CIViC)

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

Forty-seven patients with relapsed/refractory AML or 60+ years old with untreated AML were enrolled on a phase II study. In FLT3 wild-type patients, six out of 36 (17%) had a response (1 PR, 3 MR, 2 u… (full text at CIViC)

PMID 24178622 · Jain et al., 2014 · Open in CIViC

Sorafenib is effective in patients with FLT3 internal tandem repeats, but not in wild type or D835 mutation.

PMID 18230792 · Zhang et al., 2008 · Open in CIViC

13 patients with relapsed or chemo-refractory FLT3-ITD+ AML were treated with sorafenib (200-400 mg twice daily). 12 patients showed clearance or near clearance of bone marrow myeloblasts after 27 (ra… (full text at CIViC)

PMID 22368270 · Man et al., 2012 · Open in CIViC

Six children with relapsed or refractory FLT3-ITD-positive AML received initial therapy with sorafenib (alone or in combination with clofarabine and cytarabine). Four of the patients initially achiev… (full text at CIViC)

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

In a preclinical trial, MV4-11 leukemic cell lines with the FLT3-ITD mutation and RS4;11 leukemic cell lines with the native FLT3 gene were treated with the tyrosine kinase inhibitors (TKI) ponatinib,… (full text at CIViC)

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

In a preclinical trial, MV4-11 leukemic cell lines with the FLT3-ITD mutation and RS4;11 leukemic cell lines with the native FLT3 gene were treated with the tyrosine kinase inhibitors (TKI) ponatinib,… (full text at CIViC)

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

The SORMAIN trial provides evidence that an inhibition of FLT3 through sorafenib significantly reduces the risk of relapse and death after allogeneic hematopoietic stem cell transplantation for FLT3-I… (full text at CIViC)

PMID 32673171 · Burchert et al., 2020 · Open in CIViC

In a preclinical trial, the leukemic cell line MV4-11 with the FLT3-ITD mutation and the leukemic cell line RS4;11 with the native FLT3 gene were treated with the tyrosine kinase inhibitors (TKI) pona… (full text at CIViC)

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

Ba/F3 cells with both FLT3-ITD and TKD mutations on the same allele have more resistance to the protein tyrosine kinase (PTK) inhibitor SU5614 than cells with FLT3-ITD alone or FLT3 ITD and TKD mutati… (full text at CIViC)

PMID 15626738 · Bagrintseva et al., 2005 · Open in CIViC

In a preclinical trial, MV4-11 leukemic cell lines with the FLT3-ITD mutation and RS4;11 leukemic cell lines with the native FLT3 gene were treated with the tyrosine kinase inhibitors (TKI) ponatinib,… (full text at CIViC)

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

ATRA treatment did not effect overall survival in patients <60 years old with FLT3-ITD mutation.

PMID 19965647 · Burnett et al., 2010 · Open in CIViC

AG1296 is effective in triggering apoptosis in Ba/F3 and primary AML cells with FLT3 internal tandem repeat.

PMID 12357354 · Tse et al., 2002 · Open in CIViC

To identify the mutational spectrum associated with relapse, whole-exome sequencing was performed on 13 matched diagnosis, relapse, and remission trios followed by targeted sequencing of 299 genes in … (full text at CIViC)

PMID 26438511 · Garg et al., 2015 · Open in CIViC

In this phase III, randomized trial, 371 patients with Relapsed or Refractory FLT3-Mutated AML were randomized 2:1 to receive either gilteritinib (at a dose of 120 mg per day) or salvage chemotherapy.… (full text at CIViC)

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

In this phase 3 trial (ADMIRAL), 371 patients with relapsed or refractory FLT3-mutated AML (required to have FLT3 ITD or TKD D835 or I836 mutations) were randomly assigned in a 2:1 ratio to receive ei… (full text at CIViC)

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

In a trial with 13 patients with relapsed or refractory FLT3-ITD AML, considered unfit for further induction chemotherapy, D835Y emerged during resistance in three cases with initial sorafenib respons… (full text at CIViC)

PMID 22368270 · Man et al., 2012 · Open in CIViC

Using molecular docking simulations, the authors computationally screened a library of clinical compounds and identified KX2-391(Tirbanibulin, an SRC/tubulin dual inhibitor) to be a candidate FLT3 inh… (full text at CIViC)

PMID 34217323 · Wang et al., 2021 · Open in CIViC

FLT3-ITD positive AML cells with lower KDM6A expression showed sensitivity to olaparib.

Open in CIViC

Murine pro-B lymphocyte lines Ba/F3 cells with FLT3-ITD were exposed to sorafenib with increasing low doses (i.e., 1-5 nmol/L) of sorafenib for up to 3 months, and further exposed for an additional 3 … (full text at CIViC)

PMID 24619500 · Zhang et al., 2014 · Open in CIViC

Acute myeloid leukemia (AML) with an FLT3 internal tandem duplication (FLT3-ITD) mutation is an aggressive hematologic malignancy with a grave prognosis. Targeted deep sequencing was performed on FLT3… (full text at CIViC)

PMID 26438511 · Garg et al., 2015 · Open in CIViC

Proliferation of Ba/F3 cells with FLT3 double mutations was studied for the activity of ponatinib. Compared to control cells with native FLT3-ITD mutant (IC50: 3.0nM), cells with double mutants, FLT3-… (full text at CIViC)

PMID 23430109 · Smith et al., 2013 · Open in CIViC

Acute myeloid leukemia (AML) with an FLT3 internal tandem duplication (FLT3-ITD) mutation is an aggressive hematologic malignancy with a grave prognosis. Targeted deep sequencing was performed on FLT3… (full text at CIViC)

PMID 26438511 · Garg et al., 2015 · Open in CIViC

Mutations were identified by in vitro saturation mutagenesis on the background of FLT3-ITD or FLT3-ITD/F691L. Proliferation and biochemical studies showed that the FLT3-ITD D839G (IC50 =4.1μM) and FLT… (full text at CIViC)

PMID 25847190 · Smith et al., 2015 · Open in CIViC

Ningetinib inhibited Ba/F3 cells with FLT3 ITD-F691L in cell proliferation assays. FLT3-ITD-F691L cells treated with ningetinib for 6 hours demonstrated inhibition of FLT3 phosphorylation and also pho… (full text at CIViC)

PMID 38978049 · Hu et al., 2024 · Open in CIViC

Proliferation of Ba/F3 cells with FLT3 double mutations was studied for the activity of ponatinib. Compared to control cells with native FLT3-ITD mutant (IC50: 3.0nM), cells with double mutants (FLT3-… (full text at CIViC)

PMID 23430109 · Smith et al., 2013 · Open in CIViC

Murine pro-B lymphocyte lines Ba/F3 cells with FLT3-ITD were exposed to sorafenib with increasing low doses (i.e., 1-5 nmol/L) of sorafenib for up to 3 months, and further exposed for an additional 3 … (full text at CIViC)

PMID 24619500 · Zhang et al., 2014 · Open in CIViC

Acute myeloid leukemia (AML) with an FLT3 internal tandem duplication (FLT3-ITD) mutation is an aggressive hematologic malignancy with a grave prognosis. Targeted deep sequencing was performed on FLT3… (full text at CIViC)

PMID 26438511 · Garg et al., 2015 · Open in CIViC

Murine pro-B lymphocyte lines Ba/F3 cells with FLT3-ITD were exposed to sorafanib with increasing low doses (i.e., 1-5 nmol/L) of sorafenib for up to 3 months, and further exposed for an additional 3 … (full text at CIViC)

PMID 24619500 · Zhang et al., 2014 · Open in CIViC

Acute myeloid leukemia (AML) with an FLT3 internal tandem duplication (FLT3-ITD) mutation is an aggressive hematologic malignancy with a grave prognosis. Targeted deep sequencing was performed on FLT3… (full text at CIViC)

PMID 26438511 · Garg et al., 2015 · Open in CIViC

In a study looking for mechanisms of resistance within a phase 2 study using PKC412 (midostaurin), a 60 year old male with normal karyotype AML was identified with FLT3-ITD-N676K mutation. This mutati… (full text at CIViC)

PMID 16150941 · Heidel et al., 2006 · Open in CIViC

Using a saturation mutagenesis screen, resistant clones harboring N841K were identified in a Ba/F3 proliferation assay when exposed to PLX3397 on a FLT3-ITD + F691L background (Figure 3B). The N841K m… (full text at CIViC)

PMID 25847190 · Smith et al., 2015 · Open in CIViC

In a preclinical genomic and functional study of pediatric acute lymphoblastic leukemia (n = 81 paired diagnosis–relapse samples), recurrent RAS-pathway mutations involving NRAS (exons 2-3), KRAS (exo… (full text at CIViC)

PMID 24316979 · Wong et al., 2014 · Open in CIViC

A Phase III Randomized, Double-Blind study of chemotherapy + Midostaurin or Placebo in newly diagnosed patients < 60 Years of age with FLT3 mutated Acute Myeloid Leukemia (AML). Overall survival was s… (full text at CIViC)

PMID 28644114 · Stone et al., 2017 · Open in CIViC

Murine pro-B lymphocyte lines Ba/F3 cells with FLT3-ITD were exposed to sorafenib with increasing low doses (i.e., 1-5 nmol/L) of sorafenib for up to 3 months, and further exposed for an additional 3 … (full text at CIViC)

PMID 24619500 · Zhang et al., 2014 · Open in CIViC

Acute myeloid leukemia (AML) with an FLT3 internal tandem duplication (FLT3-ITD) mutation is an aggressive hematologic malignancy with a grave prognosis. Targeted deep sequencing was performed on FLT3… (full text at CIViC)

PMID 26438511 · Garg et al., 2015 · Open in CIViC

By assessing cell viability using MTS assay, FF-10101 showed growth inhibitory effects on FLT3-ITD with Y842C mutation expressing 32D cells(Figure 3A). Consistently, FF-10101 potently inhibited FLT3 p… (full text at CIViC)

PMID 29187377 · Yamaura et al., 2018 · Open in CIViC

Proliferation of Ba/F3 cells with FLT3 double mutations was studied for the activity of ponatinib and sorafenib. Compared to control cells with native FLT3-ITD mutant (IC50: 3.0nM), cells with double … (full text at CIViC)

PMID 23430109 · Smith et al., 2013 · Open in CIViC

From 109 unselected AML patients, one was identified to harbor a FLT3 K663Q mutation in the TK1 domain [outside the juxtamembrane (JM) domain and the activation loop (AL)], homologous to the KIT K642E… (full text at CIViC)

PMID 16990784 · Schittenhelm et al., 2006 · Open in CIViC

Mutations were identified by in vitro saturation mutagenesis on the background of FLT3-ITD or FLT3-ITD/F691L. Proliferation and biochemical studies showed that the FLT3-ITD M664I (IC50 =0.61μM) and FL… (full text at CIViC)

PMID 25847190 · Smith et al., 2015 · Open in CIViC

FLT3 M737I variant was found in patient at diagnosis but absent in the remission sample. BaF3 cells was transformed to express M737I and these cells were unable to grow in the absence of IL-3 similar … (full text at CIViC)

PMID 18068628 · Fröhling et al., 2007 · Open in CIViC

In this cohort, 431 patients (537 specimens underwent targeted NGS, 68 patients underwent more than one sequencing reaction) with an AML diagnosis (new and r/r) were analyzed to identify and character… (full text at CIViC)

PMID 30181385 · Schwartz et al., 2019 · Open in CIViC

FLT3 mutations did not alter overall survival or remission duration in younger (16-60), cytogenetically normal AML patients with CEBPA mutations. 10/36 patients with CEBPA mutations also had FLT3 muta… (full text at CIViC)

PMID 14726504 · Fröhling et al., 2004 · Open in CIViC