A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

The Biochemical journal 20130415

Small-molecule screen identifies modulators of EWS/FLI1 target gene expression and cell survival in Ewing's sarcoma.

International journal of cancer 20121101

Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors.

Leukemia 20121001

Phase IB study of the FLT3 kinase inhibitor midostaurin with chemotherapy in younger newly diagnosed adult patients with acute myeloid leukemia.

Leukemia 20120901

Individual dose and scheduling determine the efficacy of combining cytotoxic anticancer agents with a kinase inhibitor in non-small-cell lung cancer.

Journal of cancer research and clinical oncology 20120801

Midostaurin does not prolong cardiac repolarization defined in a thorough electrocardiogram trial in healthy volunteers.

Cancer chemotherapy and pharmacology 20120501

Systemic mastocytosis in adults: 2012 Update on diagnosis, risk stratification, and management.

American journal of hematology 20120401

Molecular targeted therapy in acute myeloid leukemia.

Hematology (Amsterdam, Netherlands) 20120401

Tetracyclines convert the osteoclastic-differentiation pathway of progenitor cells to produce dendritic cell-like cells.

Journal of immunology (Baltimore, Md. : 1950) 20120215

KIT with D816 mutations cooperates with CBFB-MYH11 for leukemogenesis in mice.

Blood 20120209

VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.

Journal of medicinal chemistry 20120126

H2O2 production downstream of FLT3 is mediated by p22phox in the endoplasmic reticulum and is required for STAT5 signalling.

PloS one 20120101

Clinical experience with antiangiogenic therapy in leukemia.

Current cancer drug targets 20111101

Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

Nature biotechnology 20111101

Comprehensive analysis of kinase inhibitor selectivity.

Nature biotechnology 20111030

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 of medicinal chemistry 20111027

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.

Journal of medicinal chemistry 20111027

Tyrosine kinase inhibitors in the treatment of systemic mastocytosis.

Leukemia research 20110901

KIT-D816V-independent oncogenic signaling in neoplastic cells in systemic mastocytosis: role of Lyn and Btk activation and disruption by dasatinib and bosutinib.

Blood 20110818

FLT3 inhibition as therapy in acute myeloid leukemia: a record of trials and tribulations.

The oncologist 20110801

Up-regulation of homeodomain genes, DLX1 and DLX2, by FLT3 signaling.

Haematologica 20110601

Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.

European journal of medicinal chemistry 20110601

Systemic mastocytosis in adults: 2011 update on diagnosis, risk stratification, and management.

American journal of hematology 20110401

KIT signaling regulates MITF expression through miRNAs in normal and malignant mast cell proliferation.

Blood 20110331

FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo.

Blood 20110324

Effects of the protein kinase inhibitor PKC412 on gene expression and link to physiological effects in zebrafish Danio rerio eleuthero-embryos.

Toxicological sciences : an official journal of the Society of Toxicology 20110101

Reversible resistance induced by FLT3 inhibition: a novel resistance mechanism in mutant FLT3-expressing cells.

PloS one 20110101

Smac mimetics: implications for enhancement of targeted therapies in leukemia.

Leukemia 20101201

Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.

Chemistry & biology 20101124

Critical role for hyperpolarization-activated cyclic nucleotide-gated channel 2 in the AIF-mediated apoptosis.

The EMBO journal 20101117

H1-receptor antagonists terfenadine and loratadine inhibit spontaneous growth of neoplastic mast cells.

Experimental hematology 20101001

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 of clinical oncology : official journal of the American Society of Clinical Oncology 20101001

Midostaurin (PKC412) modulates differentiation and maturation of human myeloid dendritic cells.

Toxicology in vitro : an international journal published in association with BIBRA 20100901

p21 Downregulation is an important component of PAX3/FKHR oncogenicity and its reactivation by HDAC inhibitors enhances combination treatment.

Oncogene 20100708

Mechanisms of resistance against PKC412 in resistant FLT3-ITD positive human acute myeloid leukemia cells.

Annals of hematology 20100701

Combining the FLT3 inhibitor PKC412 and the triterpenoid CDDO-Me synergistically induces apoptosis in acute myeloid leukemia with the internal tandem duplication mutation.

Molecular cancer research : MCR 20100701

Interactive medical case. A rash hypothesis.

The New England journal of medicine 20100617

[FLT3 kinase inhibitors for the treatment of acute leukemia].

[Rinsho ketsueki] The Japanese journal of clinical hematology 20100601

Maintenance therapy in acute myeloid leukemia revisited: will new agents rekindle an old interest?

Current opinion in hematology 20100301

Colony stimulating factor-1 receptor as a target for small molecule inhibitors.

Bioorganic & medicinal chemistry 20100301

FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML.

Blood 20100218

Randomized clinical trials with biomarkers: design issues.

Journal of the National Cancer Institute 20100203

Identification of proapoptotic Bim as a tumor suppressor in neoplastic mast cells: role of KIT D816V and effects of various targeted drugs.

Blood 20091217

Growth-inhibitory effects of four tyrosine kinase inhibitors on neoplastic feline mast cells exhibiting a Kit exon 8 ITD mutation.

Veterinary immunology and immunopathology 20091215

FLT3 inhibition as a targeted therapy for acute myeloid leukemia.

Current opinion in oncology 20091101

Midostaurin (PKC412) inhibits immunoglobulin E-dependent activation and mediator release in human blood basophils and mast cells.

Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology 20091101

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Blood 20091001

Oral small-molecule tyrosine kinase inhibitor midostaurin (PKC412) inhibits growth and induces megakaryocytic differentiation in human leukemia cells.

Toxicology in vitro : an international journal published in association with BIBRA 20090901

A novel molecular mechanism of primary resistance to FLT3-kinase inhibitors in AML.

Blood 20090423

FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro.

Cancer research 20090401

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.

Blood 20090305

Bis(1H-indol-2-yl)methanones are effective inhibitors of FLT3-ITD tyrosine kinase and partially overcome resistance to PKC412A in vitro.

British journal of haematology 20090301

Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells.

Blood 20081215

Peptide biosensors for the electrochemical measurement of protein kinase activity.

Analytical chemistry 20081215

Existing and emerging therapeutic options for the treatment of acute myeloid leukemia.

Clinical advances in hematology & oncology : H&O 20081101

New agents for the treatment of AML recent study findings.

Clinical advances in hematology & oncology : H&O 20081101

Future research directions for the treatment of AML.

Clinical advances in hematology & oncology : H&O 20081101

Oncostatin M induces bone loss and sensitizes rat osteosarcoma to the antitumor effect of Midostaurin in vivo.

Clinical cancer research : an official journal of the American Association for Cancer Research 20080901

The FLT3 inhibitor PKC412 in combination with cytostatic drugs in vitro in acute myeloid leukemia.

Cancer chemotherapy and pharmacology 20080801

Dose- and time-dependent pharmacokinetics of midostaurin in patients with diabetes mellitus.

Journal of clinical pharmacology 20080601

The FLT3 inhibitor PKC412 exerts differential cell cycle effects on leukemic cells depending on the presence of FLT3 mutations.

Oncogene 20080515

Phosphorylation regulates transcriptional activity of PAX3/FKHR and reveals novel therapeutic possibilities.

Cancer research 20080515

A quantitative analysis of kinase inhibitor selectivity.

Nature biotechnology 20080101

[Gastrointestinal stromal tumors: molecular aspects and therapeutic implications].

Bulletin du cancer 20080101

Inhibition of PKCalpha activation in human bone and soft tissue sarcoma cells by the selective PKC inhibitor PKC412.

Anticancer research 20080101

[Protein kinases C: a new cytoplasmic target].

Bulletin du cancer 20080101

A mechanism-based population pharmacokinetic model for characterizing time-dependent pharmacokinetics of midostaurin and its metabolites in human subjects.

Clinical pharmacokinetics 20080101

Uniform sensitivity of FLT3 activation loop mutants to the tyrosine kinase inhibitor midostaurin.

Blood 20071215

FLT3 regulates beta-catenin tyrosine phosphorylation, nuclear localization, and transcriptional activity in acute myeloid leukemia cells.

Leukemia 20071201

Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles.

Cancer cell 20071201

FLT3 kinase inhibitors in the management of acute myeloid leukemia.

Clinical lymphoma & myeloma 20071201

Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT.

Haematologica 20071101

Role of mutation independent constitutive activation of FLT3 in juvenile myelomonocytic leukemia.

Haematologica 20071101

PKC 412 small-molecule tyrosine kinase inhibitor: single-compound therapy for pancreatic cancer.

Cancer 20071001

Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations.

Experimental hematology 20071001

PKC412 (CGP41251) modulates the proliferation and lipopolysaccharide-induced inflammatory responses of RAW 264.7 macrophages.

Biochemical and biophysical research communications 20070817

Identification of heat shock protein 32 (Hsp32) as a novel survival factor and therapeutic target in neoplastic mast cells.

Blood 20070715

Potentiation of antileukemic therapies by Smac mimetic, LBW242: effects on mutant FLT3-expressing cells.

Molecular cancer therapeutics 20070701

Divergent cytotoxic effects of PKC412 in combination with conventional antileukemic agents in FLT3 mutation-positive versus -negative leukemia cell lines.

Leukemia 20070501

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.

Blood 20070401

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Molecular cancer therapeutics 20070301

PKC412 demonstrates JNK-dependent activity against human multiple myeloma cells.

Blood 20070215

[Novel molecularly target therapies for leukemia].

Nihon rinsho. Japanese journal of clinical medicine 20070128

A highly sensitive method for the detection of PKC412 (CGP41251) and its metabolites by high-performance liquid chromatography.

Journal of pharmacological and toxicological methods 20070101

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.

Leukemia 20061201

Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity.

Gastroenterology 20061201

Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors.

Blood 20061115

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.

Blood 20061115

Beyond imatinib: second generation c-KIT inhibitors for the management of gastrointestinal stromal tumors.

Clinical colorectal cancer 20061101

The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study.

British journal of cancer 20061009

Inhibitors of the PI3-kinase/Akt pathway induce mitotic catastrophe in non-small cell lung cancer cells.

International journal of cancer 20060901

Reversal of endothelial nitric oxide synthase uncoupling and up-regulation of endothelial nitric oxide synthase expression lowers blood pressure in hypertensive rats.

Journal of the American College of Cardiology 20060620

Point mutations in the juxtamembrane domain of FLT3 define a new class of activating mutations in AML.

Blood 20060501

[The present status of, and problems with the development of FLT3 kinase inhibitors].

[Rinsho ketsueki] The Japanese journal of clinical hematology 20060401

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Expert opinion on emerging drugs 20060301

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.

Blood 20060115

Clinical resistance to the kinase inhibitor PKC412 in acute myeloid leukemia by mutation of Asn-676 in the FLT3 tyrosine kinase domain.

Blood 20060101

Antitumor and normal cell protective effect of PKC412 in the athymic mouse model of ovarian cancer.

Annals of clinical and laboratory science 20060101

FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies.

Oncogene 20051215

FLT3 internal tandem duplication mutations induce myeloproliferative or lymphoid disease in a transgenic mouse model.

Oncogene 20051124

Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation.

Blood 20051015

Targeting FLT3 in primary MLL-gene-rearranged infant acute lymphoblastic leukemia.

Blood 20051001

Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412.

Blood 20050715

AML-associated Flt3 kinase domain mutations show signal transduction differences compared with Flt3 ITD mutations.

Blood 20050701

Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activation and TNF-alpha production.

International immunopharmacology 20050701

FLT3 inhibition in t(4;11)+ adult acute lymphoid leukaemia.

British journal of haematology 20050701

Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse.

Nitric oxide : biology and chemistry 20050601

N-benzoylstaurosporine (PKC412) inhibits Akt kinase inducing apoptosis in multiple myeloma cells.

Leukemia & lymphoma 20050601

The hypereosinophilic syndrome: idiopathic or not, that is the question.

Haematologica 20050501

PKC 412 sensitizes U1810 non-small cell lung cancer cells to DNA damage.

Experimental cell research 20050415

[Possibility of targeting FLT3 kinase for the treatment of leukemia].

[Rinsho ketsueki] The Japanese journal of clinical hematology 20050301

[New targets for molecular therapy of acute leukemia: a 'single-hit' or 'multiple-hit' strategy against signaling pathway].

Zhonghua yi xue za zhi 20050223

Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants.

Gastroenterology 20050201

Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412.

Blood 20050101

New concepts in the treatment of acute myeloid malignancies: selected pathways for targeted therapy.

Journal of biological regulators and homeostatic agents 20050101

Inhibitory effect of epidermal growth factor on resveratrol-induced apoptosis in prostate cancer cells is mediated by protein kinase C-alpha.

Molecular cancer therapeutics 20041101

Identifying and characterizing a novel activating mutation of the FLT3 tyrosine kinase in AML.

Blood 20040915

Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia.

Cancer research 20040915

PKC412 induces apoptosis through a caspase-dependent mechanism in human keloid-derived fibroblasts.

European journal of pharmacology 20040823

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.

Clinical cancer research : an official journal of the American Association for Cancer Research 20040801

Evidence for contribution of vascular NAD(P)H oxidase to increased oxidative stress in animal models of diabetes and obesity.

Free radical biology & medicine 20040701

Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3.

Cancer research 20040515

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.

Investigational new drugs 20040401

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.

Blood 20040315

Reduction of diabetic macular edema by oral administration of the kinase inhibitor PKC412.

Investigative ophthalmology & visual science 20040301

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?

International journal of radiation oncology, biology, physics 20040201

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.

Annals of oncology : official journal of the European Society for Medical Oncology 20040201

Periocular injection of microspheres containing PKC412 inhibits choroidal neovascularization in a porcine model.

Investigative ophthalmology & visual science 20031101

Prostacyclin production in rat aortic smooth muscle cells: role of protein kinase C, phospholipase D and cyclooxygenase-2 expression.

Cardiovascular research 20031101

The kinase inhibitor PKC412 suppresses epiretinal membrane formation and retinal detachment in mice with proliferative retinopathies.

Investigative ophthalmology & visual science 20030801

Sensitivity toward tyrosine kinase inhibitors varies between different activating mutations of the FLT3 receptor.

Blood 20030715

PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease.

Cancer cell 20030501

Effect of PKC412, a selective inhibitor of protein kinase C, on lung metastasis in mice injected with B16 melanoma cells.

Life sciences 20030207

Inhibition of FLT3 in MLL. Validation of a therapeutic target identified by gene expression based classification.

Cancer cell 20030201

Effect of PKC412, an inhibitor of protein kinase C, on spontaneous metastatic model mice.

Anticancer research 20030101

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.

Cancer chemotherapy and pharmacology 20020601

Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412.

Cancer cell 20020601

Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro.

Haematologica 20020201

Protein kinase C inhibitors.

Current oncology reports 20020101

A novel treatment approach for low grade lymphoproliferative disorders using PKC412 (CGP41251), an inhibitor of protein kinase C.

The hematology journal : the official journal of the European Haematology Association 20020101

The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C.

Cancer research 20011115

In vitro prevention of the emergence of multidrug resistance in a pediatric rhabdomyosarcoma cell line.

Clinical cancer research : an official journal of the American Association for Cancer Research 20011001

CGP 41251, a new potential anticancer drug, improves contractility of rat isolated cardiac muscle subjected to hypoxia.

Journal of cardiovascular pharmacology 20010601

Phase I and pharmacokinetic study of PKC412, an inhibitor of protein kinase C.

Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20010301

Differential p53-dependent mechanism of radiosensitization in vitro and in vivo by the protein kinase C-specific inhibitor PKC412.

Cancer research 20010115

Analogs of staurosporine: potential anticancer drugs?

General pharmacology 19981101

Differential inhibition of cytosolic and membrane-derived protein kinase C activity by staurosporine and other kinase inhibitors.

FEBS letters 19950403