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Title: Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors.
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Title: Phase IB study of the FLT3 kinase inhibitor midostaurin with chemotherapy in younger newly diagnosed adult patients with acute myeloid leukemia.
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Title: Individual dose and scheduling determine the efficacy of combining cytotoxic anticancer agents with a kinase inhibitor in non-small-cell lung cancer.
Journal: Journal of cancer research and clinical oncology20120801
Title: Midostaurin does not prolong cardiac repolarization defined in a thorough electrocardiogram trial in healthy volunteers.
Journal: Cancer chemotherapy and pharmacology20120501
Title: Systemic mastocytosis in adults: 2012 Update on diagnosis, risk stratification, and management.
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Title: Tetracyclines convert the osteoclastic-differentiation pathway of progenitor cells to produce dendritic cell-like cells.
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Title: KIT with D816 mutations cooperates with CBFB-MYH11 for leukemogenesis in mice.
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Title: VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.
Journal: Journal of medicinal chemistry20120126
Title: H2O2 production downstream of FLT3 is mediated by p22phox in the endoplasmic reticulum and is required for STAT5 signalling.
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Title: Clinical experience with antiangiogenic therapy in leukemia.
Journal: Current cancer drug targets20111101
Title: Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.
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Title: Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Journal: Journal of medicinal chemistry20111027
Title: Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.
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Title: Tyrosine kinase inhibitors in the treatment of systemic mastocytosis.
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Title: KIT-D816V-independent oncogenic signaling in neoplastic cells in systemic mastocytosis: role of Lyn and Btk activation and disruption by dasatinib and bosutinib.
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Title: FLT3 inhibition as therapy in acute myeloid leukemia: a record of trials and tribulations.
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Title: Up-regulation of homeodomain genes, DLX1 and DLX2, by FLT3 signaling.
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Title: Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
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Title: Systemic mastocytosis in adults: 2011 update on diagnosis, risk stratification, and management.
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Title: KIT signaling regulates MITF expression through miRNAs in normal and malignant mast cell proliferation.
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Title: FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo.
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Title: Effects of the protein kinase inhibitor PKC412 on gene expression and link to physiological effects in zebrafish Danio rerio eleuthero-embryos.
Journal: Toxicological sciences : an official journal of the Society of Toxicology20110101
Title: Reversible resistance induced by FLT3 inhibition: a novel resistance mechanism in mutant FLT3-expressing cells.
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Title: Smac mimetics: implications for enhancement of targeted therapies in leukemia.
Journal: Leukemia20101201
Title: Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
Journal: Chemistry & biology20101124
Title: Critical role for hyperpolarization-activated cyclic nucleotide-gated channel 2 in the AIF-mediated apoptosis.
Journal: The EMBO journal20101117
Title: H1-receptor antagonists terfenadine and loratadine inhibit spontaneous growth of neoplastic mast cells.
Journal: Experimental hematology20101001
Title: Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3.
Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology20101001
Title: Midostaurin (PKC412) modulates differentiation and maturation of human myeloid dendritic cells.
Journal: Toxicology in vitro : an international journal published in association with BIBRA20100901
Title: p21 Downregulation is an important component of PAX3/FKHR oncogenicity and its reactivation by HDAC inhibitors enhances combination treatment.
Journal: Oncogene20100708
Title: Mechanisms of resistance against PKC412 in resistant FLT3-ITD positive human acute myeloid leukemia cells.
Journal: Annals of hematology20100701
Title: Combining the FLT3 inhibitor PKC412 and the triterpenoid CDDO-Me synergistically induces apoptosis in acute myeloid leukemia with the internal tandem duplication mutation.
Journal: Molecular cancer research : MCR20100701
Title: Interactive medical case. A rash hypothesis.
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Title: Maintenance therapy in acute myeloid leukemia revisited: will new agents rekindle an old interest?
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Title: Colony stimulating factor-1 receptor as a target for small molecule inhibitors.
Journal: Bioorganic & medicinal chemistry20100301
Title: FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML.
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Title: Randomized clinical trials with biomarkers: design issues.
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Title: Identification of proapoptotic Bim as a tumor suppressor in neoplastic mast cells: role of KIT D816V and effects of various targeted drugs.
Journal: Blood20091217
Title: Growth-inhibitory effects of four tyrosine kinase inhibitors on neoplastic feline mast cells exhibiting a Kit exon 8 ITD mutation.
Journal: Veterinary immunology and immunopathology20091215
Title: FLT3 inhibition as a targeted therapy for acute myeloid leukemia.
Journal: Current opinion in oncology20091101
Title: Midostaurin (PKC412) inhibits immunoglobulin E-dependent activation and mediator release in human blood basophils and mast cells.
Journal: Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology20091101
Title: AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Journal: Blood20091001
Title: Oral small-molecule tyrosine kinase inhibitor midostaurin (PKC412) inhibits growth and induces megakaryocytic differentiation in human leukemia cells.
Journal: Toxicology in vitro : an international journal published in association with BIBRA20090901
Title: A novel molecular mechanism of primary resistance to FLT3-kinase inhibitors in AML.
Journal: Blood20090423
Title: FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro.
Journal: Cancer research20090401
Title: BH3-only protein Bim more critical than Puma in tyrosine kinase inhibitor-induced apoptosis of human leukemic cells and transduced hematopoietic progenitors carrying oncogenic FLT3.
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Title: Bis(1H-indol-2-yl)methanones are effective inhibitors of FLT3-ITD tyrosine kinase and partially overcome resistance to PKC412A in vitro.
Journal: British journal of haematology20090301
Title: Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells.
Journal: Blood20081215
Title: Peptide biosensors for the electrochemical measurement of protein kinase activity.
Journal: Analytical chemistry20081215
Title: Existing and emerging therapeutic options for the treatment of acute myeloid leukemia.
Journal: Clinical advances in hematology & oncology : H&O20081101
Title: New agents for the treatment of AML recent study findings.
Journal: Clinical advances in hematology & oncology : H&O20081101
Title: Future research directions for the treatment of AML.
Journal: Clinical advances in hematology & oncology : H&O20081101
Title: Oncostatin M induces bone loss and sensitizes rat osteosarcoma to the antitumor effect of Midostaurin in vivo.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20080901
Title: The FLT3 inhibitor PKC412 in combination with cytostatic drugs in vitro in acute myeloid leukemia.
Journal: Cancer chemotherapy and pharmacology20080801
Title: Dose- and time-dependent pharmacokinetics of midostaurin in patients with diabetes mellitus.
Journal: Journal of clinical pharmacology20080601
Title: The FLT3 inhibitor PKC412 exerts differential cell cycle effects on leukemic cells depending on the presence of FLT3 mutations.
Journal: Oncogene20080515
Title: Phosphorylation regulates transcriptional activity of PAX3/FKHR and reveals novel therapeutic possibilities.
Journal: Cancer research20080515
Title: A quantitative analysis of kinase inhibitor selectivity.
Journal: Nature biotechnology20080101
Title: [Gastrointestinal stromal tumors: molecular aspects and therapeutic implications].
Journal: Bulletin du cancer20080101
Title: Inhibition of PKCalpha activation in human bone and soft tissue sarcoma cells by the selective PKC inhibitor PKC412.
Journal: Anticancer research20080101
Title: [Protein kinases C: a new cytoplasmic target].
Journal: Bulletin du cancer20080101
Title: A mechanism-based population pharmacokinetic model for characterizing time-dependent pharmacokinetics of midostaurin and its metabolites in human subjects.
Journal: Clinical pharmacokinetics20080101
Title: Uniform sensitivity of FLT3 activation loop mutants to the tyrosine kinase inhibitor midostaurin.
Journal: Blood20071215
Title: FLT3 regulates beta-catenin tyrosine phosphorylation, nuclear localization, and transcriptional activity in acute myeloid leukemia cells.
Journal: Leukemia20071201
Title: Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles.
Journal: Cancer cell20071201
Title: FLT3 kinase inhibitors in the management of acute myeloid leukemia.
Journal: Clinical lymphoma & myeloma20071201
Title: Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT.
Journal: Haematologica20071101
Title: Role of mutation independent constitutive activation of FLT3 in juvenile myelomonocytic leukemia.
Journal: Haematologica20071101
Title: PKC 412 small-molecule tyrosine kinase inhibitor: single-compound therapy for pancreatic cancer.
Journal: Cancer20071001
Title: Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations.
Journal: Experimental hematology20071001
Title: PKC412 (CGP41251) modulates the proliferation and lipopolysaccharide-induced inflammatory responses of RAW 264.7 macrophages.
Journal: Biochemical and biophysical research communications20070817
Title: Identification of heat shock protein 32 (Hsp32) as a novel survival factor and therapeutic target in neoplastic mast cells.
Journal: Blood20070715
Title: Potentiation of antileukemic therapies by Smac mimetic, LBW242: effects on mutant FLT3-expressing cells.
Journal: Molecular cancer therapeutics20070701
Title: Divergent cytotoxic effects of PKC412 in combination with conventional antileukemic agents in FLT3 mutation-positive versus -negative leukemia cell lines.
Journal: Leukemia20070501
Title: Identification of MCL1 as a novel target in neoplastic mast cells in systemic mastocytosis: inhibition of mast cell survival by MCL1 antisense oligonucleotides and synergism with PKC412.
Journal: Blood20070401
Title: Resistance to c-KIT kinase inhibitors conferred by V654A mutation.
Journal: Molecular cancer therapeutics20070301
Title: PKC412 demonstrates JNK-dependent activity against human multiple myeloma cells.
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Journal: Nihon rinsho. Japanese journal of clinical medicine20070128
Title: A highly sensitive method for the detection of PKC412 (CGP41251) and its metabolites by high-performance liquid chromatography.
Journal: Journal of pharmacological and toxicological methods20070101
Title: DNA repair contributes to the drug-resistant phenotype of primary acute myeloid leukaemia cells with FLT3 internal tandem duplications and is reversed by the FLT3 inhibitor PKC412.
Journal: Leukemia20061201
Title: Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity.
Journal: Gastroenterology20061201
Title: Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors.
Journal: Blood20061115
Title: The effects of lestaurtinib (CEP701) and PKC412 on primary AML blasts: the induction of cytotoxicity varies with dependence on FLT3 signaling in both FLT3-mutated and wild-type cases.
Journal: Blood20061115
Title: Beyond imatinib: second generation c-KIT inhibitors for the management of gastrointestinal stromal tumors.
Journal: Clinical colorectal cancer20061101
Title: The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study.
Journal: British journal of cancer20061009
Title: Inhibitors of the PI3-kinase/Akt pathway induce mitotic catastrophe in non-small cell lung cancer cells.
Journal: International journal of cancer20060901
Title: Reversal of endothelial nitric oxide synthase uncoupling and up-regulation of endothelial nitric oxide synthase expression lowers blood pressure in hypertensive rats.
Journal: Journal of the American College of Cardiology20060620
Title: Point mutations in the juxtamembrane domain of FLT3 define a new class of activating mutations in AML.
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Journal: Expert opinion on emerging drugs20060301
Title: PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects.
Journal: Blood20060115
Title: Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain.
Journal: Blood20060101
Title: Antitumor and normal cell protective effect of PKC412 in the athymic mouse model of ovarian cancer.
Journal: Annals of clinical and laboratory science20060101
Title: FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies.
Journal: Oncogene20051215
Title: FLT3 internal tandem duplication mutations induce myeloproliferative or lymphoid disease in a transgenic mouse model.
Journal: Oncogene20051124
Title: Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation.
Journal: Blood20051015
Title: Targeting FLT3 in primary MLL-gene-rearranged infant acute lymphoblastic leukemia.
Journal: Blood20051001
Title: Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412.
Journal: Blood20050715
Title: AML-associated Flt3 kinase domain mutations show signal transduction differences compared with Flt3 ITD mutations.
Journal: Blood20050701
Title: Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activation and TNF-alpha production.
Journal: International immunopharmacology20050701
Title: FLT3 inhibition in t(4;11)+ adult acute lymphoid leukaemia.
Journal: British journal of haematology20050701
Title: Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse.
Journal: Nitric oxide : biology and chemistry20050601
Title: N-benzoylstaurosporine (PKC412) inhibits Akt kinase inducing apoptosis in multiple myeloma cells.
Journal: Leukemia & lymphoma20050601
Title: The hypereosinophilic syndrome: idiopathic or not, that is the question.
Journal: Haematologica20050501
Title: PKC 412 sensitizes U1810 non-small cell lung cancer cells to DNA damage.
Journal: Experimental cell research20050415
Title: [Possibility of targeting FLT3 kinase for the treatment of leukemia].
Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology20050301
Title: [New targets for molecular therapy of acute leukemia: a 'single-hit' or 'multiple-hit' strategy against signaling pathway].
Journal: Zhonghua yi xue za zhi20050223
Title: Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants.
Journal: Gastroenterology20050201
Title: Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412.
Journal: Blood20050101
Title: New concepts in the treatment of acute myeloid malignancies: selected pathways for targeted therapy.
Journal: Journal of biological regulators and homeostatic agents20050101
Title: Inhibitory effect of epidermal growth factor on resveratrol-induced apoptosis in prostate cancer cells is mediated by protein kinase C-alpha.
Journal: Molecular cancer therapeutics20041101
Title: Identifying and characterizing a novel activating mutation of the FLT3 tyrosine kinase in AML.
Journal: Blood20040915
Title: Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia.
Journal: Cancer research20040915
Title: PKC412 induces apoptosis through a caspase-dependent mechanism in human keloid-derived fibroblasts.
Journal: European journal of pharmacology20040823
Title: Superior activity of the combination of histone deacetylase inhibitor LAQ824 and the FLT-3 kinase inhibitor PKC412 against human acute myelogenous leukemia cells with mutant FLT-3.
Journal: Clinical cancer research : an official journal of the American Association for Cancer Research20040801
Title: Evidence for contribution of vascular NAD(P)H oxidase to increased oxidative stress in animal models of diabetes and obesity.
Journal: Free radical biology & medicine20040701
Title: Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3.
Journal: Cancer research20040515
Title: A phase I trial of daily oral 4'- N -benzoyl-staurosporine in combination with protracted continuous infusion 5-fluorouracil in patients with advanced solid malignancies.
Journal: Investigational new drugs20040401
Title: Mutations in the tyrosine kinase domain of FLT3 define a new molecular mechanism of acquired drug resistance to PTK inhibitors in FLT3-ITD-transformed hematopoietic cells.
Journal: Blood20040315
Title: Reduction of diabetic macular edema by oral administration of the kinase inhibitor PKC412.
Journal: Investigative ophthalmology & visual science20040301
Title: Novel radiosensitizers for locally advanced epithelial tumors: inhibition of the PI3K/Akt survival pathway in tumor cells and in tumor-associated endothelial cells as a novel treatment strategy?
Journal: International journal of radiation oncology, biology, physics20040201
Title: Phase I study of PKC412 (N-benzoyl-staurosporine), a novel oral protein kinase C inhibitor, combined with gemcitabine and cisplatin in patients with non-small-cell lung cancer.
Journal: Annals of oncology : official journal of the European Society for Medical Oncology20040201
Title: Periocular injection of microspheres containing PKC412 inhibits choroidal neovascularization in a porcine model.
Journal: Investigative ophthalmology & visual science20031101
Title: Prostacyclin production in rat aortic smooth muscle cells: role of protein kinase C, phospholipase D and cyclooxygenase-2 expression.
Journal: Cardiovascular research20031101
Title: The kinase inhibitor PKC412 suppresses epiretinal membrane formation and retinal detachment in mice with proliferative retinopathies.
Journal: Investigative ophthalmology & visual science20030801
Title: Sensitivity toward tyrosine kinase inhibitors varies between different activating mutations of the FLT3 receptor.
Journal: Blood20030715
Title: PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease.
Journal: Cancer cell20030501
Title: Effect of PKC412, a selective inhibitor of protein kinase C, on lung metastasis in mice injected with B16 melanoma cells.
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Title: Inhibition of FLT3 in MLL. Validation of a therapeutic target identified by gene expression based classification.
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Title: Effect of PKC412, an inhibitor of protein kinase C, on spontaneous metastatic model mice.
Journal: Anticancer research20030101
Title: A protein kinase C inhibitor induces phenotypic reversion of ras-transformed pancreatic cancer cells and cooperatively blocks tumor cell proliferation with an anti- ras peptide.
Journal: Cancer chemotherapy and pharmacology20020601
Title: Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412.
Journal: Cancer cell20020601
Title: Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro.
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Title: The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C.
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Title: CGP 41251, a new potential anticancer drug, improves contractility of rat isolated cardiac muscle subjected to hypoxia.
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