JAK2 inhibition for the treatment of hematologic and solid malignancies

No evidence for JAK2 V617F mutation in colorectal cancer

(2018) M. Herreros-Villanueva et al.   BRITISH JOURNAL OF BIOMEDICAL SCIENCE

Phase II study of SB1518, an orally available novel JAK2 inhibitor, in patients with myelofibrosis.

(2017) H. J. Deeg et al.   JOURNAL OF CLINICAL ONCOLOGY

Activating Mutation (V617F) in the Tyrosine Kinase JAK2 is Absent in Locally-Confined or Castration-Resistant Prostate Cancer

(2015) Lei Gu et al.   Analytical Cellular Pathology

TG-101348

(2014) B.L. Harry et al.   DRUGS OF THE FUTURE

A Double-Blind, Placebo-Controlled Trial of Ruxolitinib for Myelofibrosis

(2012) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

JAK Inhibition with Ruxolitinib versus Best Available Therapy for Myelofibrosis

(2012) Claire Harrison et al.   NEW ENGLAND JOURNAL OF MEDICINE

The JAK2 exon 12 mutations: A comprehensive review

(2011) Linda M. Scott   AMERICAN JOURNAL OF HEMATOLOGY

JAK2 rearrangements, including the novel SEC31A-JAK2 fusion, are recurrent in classical Hodgkin lymphoma

(2011) K. Van Roosbroeck et al.   BLOOD

Results from a randomized trial of salvage chemotherapy followed by lestaurtinib for patients with FLT3 mutant AML in first relapse

(2011) M. Levis et al.   BLOOD

Phase I trial of lestaurtinib for children with refractory neuroblastoma: a new approaches to neuroblastoma therapy consortium study

(2011) Jane E. Minturn et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Preclinical evaluation of lestaurtinib (CEP-701) in combination with retinoids for neuroblastoma

(2011) Robin E. Norris et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Celecoxib Inhibits Interleukin-6/Interleukin-6 Receptor-Induced JAK2/STAT3 Phosphorylation in Human Hepatocellular Carcinoma Cells

(2011) Y. Liu et al.   Cancer Prevention Research

Antiangiogenic and Antimetastatic Activity of JAK Inhibitor AZD1480

(2011) H. Xin et al.   CANCER RESEARCH

STAT3 Plays a Critical Role in KRAS-Induced Pancreatic Tumorigenesis

(2011) R. B. Corcoran et al.   CANCER RESEARCH

Aurora B kinase inhibition in mitosis: Strategies for optimizing the use of Aurora kinase inhibitors such as AT9283

(2011) Jayne Curry et al.   CELL CYCLE

Antimyeloma Activity of a Multitargeted Kinase Inhibitor, AT9283, via Potent Aurora Kinase and STAT3 Inhibition Either Alone or in Combination with Lenalidomide

(2011) L. Santo et al.   CLINICAL CANCER RESEARCH

STAT5A-Mediated SOCS2 Expression Regulates Jak2 and STAT3 Activity Following c-Src Inhibition in Head and Neck Squamous Carcinoma

(2011) B. Sen et al.   CLINICAL CANCER RESEARCH

New JAK2 inhibitors for myeloproliferative neoplasms

(2011) Alfonso Quintás-Cardama et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Human gastrin mRNA expression up-regulated by Helicobacter pylori CagA through MEK/ERK and JAK2-signaling pathways in gastric cancer cells

(2011) Jianjiang Zhou et al.   Gastric Cancer

Expression of p-JAK2 predicts clinical outcome and is a potential molecular target of acute myelogenous leukemia

(2011) Takayuki Ikezoe et al.   INTERNATIONAL JOURNAL OF CANCER

Safety and Efficacy of TG101348, a Selective JAK2 Inhibitor, in Myelofibrosis

(2011) Animesh Pardanani et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery of the Macrocycle 11-(2-Pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a Potent Janus Kinase 2/Fms-Like Tyrosine Kinase-3 (JAK2/FLT3) Inhibitor for the Treatment of Myelofibrosis and Lymphoma

(2011) Anthony D. William et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of JAK2 Signaling by TG101209 Enhances Radiotherapy in Lung Cancer Models

(2011) Yunguang Sun et al.   Journal of Thoracic Oncology

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2

(2011) A V Purandare et al.   LEUKEMIA

The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells

(2011) K A Monaghan et al.   LEUKEMIA

SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies

(2011) S Hart et al.   LEUKEMIA

JAK2/STAT3 signaling pathway activation mediates tumor angiogenesis by upregulation of VEGF and bFGF in non-small-cell lung cancer

(2011) Mei Zhao et al.   LUNG CANCER

STAT3 expression in activating EGFR-driven adenocarcinoma of the lung

(2011) Saburo Takata et al.   LUNG CANCER

Serious Adverse Events During Ruxolitinib Treatment Discontinuation in Patients With Myelofibrosis

(2011) Ayalew Tefferi et al.   MAYO CLINIC PROCEEDINGS

B7-H3 Silencing Increases Paclitaxel Sensitivity by Abrogating Jak2/Stat3 Phosphorylation

(2011) H. Liu et al.   MOLECULAR CANCER THERAPEUTICS

Therapeutic Potential of AZD1480 for the Treatment of Human Glioblastoma

(2011) B. C. McFarland et al.   MOLECULAR CANCER THERAPEUTICS

Janus kinase inhibitors for the treatment of myeloproliferative neoplasias and beyond

(2011) Alfonso Quintás-Cardama et al.   NATURE REVIEWS DRUG DISCOVERY

The pseudokinase domain of JAK2 is a dual-specificity protein kinase that negatively regulates cytokine signaling

(2011) Daniela Ungureanu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Long-Term Outcome of Treatment with Ruxolitinib in Myelofibrosis

(2011) Ayalew Tefferi et al.   NEW ENGLAND JOURNAL OF MEDICINE

The tumor-suppressor gene ARHI (DIRAS3) suppresses ovarian cancer cell migration through inhibition of the Stat3 and FAK/Rho signaling pathways

(2011) D B Badgwell et al.   ONCOGENE

MUC16 induced rapid G2/M transition via interactions with JAK2 for increased proliferation and anti-apoptosis in breast cancer cells

(2011) I Lakshmanan et al.   ONCOGENE

Anti-cancer effect of bee venom toxin and melittin in ovarian cancer cells through induction of death receptors and inhibition of JAK2/STAT3 pathway

(2011) Miran Jo et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells

(2010) Vijay Ramakrishnan et al.   AMERICAN JOURNAL OF HEMATOLOGY

Efficacy of MK-0457 and in combination with vorinostat against Philadelphia chromosome positive acute lymphoblastic leukemia cells

(2010) Seiichi Okabe et al.   ANNALS OF HEMATOLOGY

Activity of the multitargeted kinase inhibitor, AT9283, in imatinib-resistant BCR-ABL-positive leukemic cells

(2010) R. Tanaka et al.   BLOOD

Integrative analysis reveals selective 9p24.1 amplification, increased PD-1 ligand expression, and further induction via JAK2 in nodular sclerosing Hodgkin lymphoma and primary mediastinal large B-cell lymphoma

(2010) M. R. Green et al.   BLOOD

CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms

(2010) J. W. Tyner et al.   BLOOD

Multiple myeloma with concomitant JAK2-positive essential thrombocythemia post-successful autologous peripheral blood hematopoietic stem cell transplant

(2010) S G Holtan et al.   BONE MARROW TRANSPLANTATION

Genetic typing of CBL, ASXL1, RUNX1, TET2 and JAK2 in juvenile myelomonocytic leukaemia reveals a genetic profile distinct from chronic myelomonocytic leukaemia

(2010) Benoîte Pérez et al.   BRITISH JOURNAL OF HAEMATOLOGY

Recombinant Human Erythropoietin Antagonizes Trastuzumab Treatment of Breast Cancer Cells via Jak2-Mediated Src Activation and PTEN Inactivation

(2010) Ke Liang et al.   CANCER CELL

Phase I dose escalation study of MK-0457, a novel Aurora kinase inhibitor, in adult patients with advanced solid tumors

(2010) Anne M. Traynor et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

MiR-375 frequently downregulated in gastric cancer inhibits cell proliferation by targeting JAK2

(2010) Ling Ding et al.   CELL RESEARCH

Lestaurtinib Enhances the Antitumor Efficacy of Chemotherapy in Murine Xenograft Models of Neuroblastoma

(2010) R. Iyer et al.   CLINICAL CANCER RESEARCH

Janus kinase 2 inhibitors in myeloproliferative disorders

(2010) Eugenio Lucia et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

PCM1–JAK2-fusion: a potential treatment target in myelodysplastic–myeloproliferative and other hemato-lymphoid neoplasms

(2010) Sylvia Hoeller et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Inhibition of DNA methyltransferase induces G2 cell cycle arrest and apoptosis in human colorectal cancer cells via inhibition of JAK2/STAT3/STAT5 signalling

(2010) Hua Xiong et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Inhibition of the JAK-2/STAT3 signaling pathway impedes the migratory and invasive potential of human glioblastoma cells

(2010) Christian Senft et al.   JOURNAL OF NEURO-ONCOLOGY

Inhibition of JAK–STAT signaling by TG101348: a novel mechanism for inhibition of KITD816V-dependent growth in mast cell leukemia cells

(2010) T Lasho et al.   LEUKEMIA

JAK2 46/1 haplotype analysis in myeloproliferative neoplasms and acute myeloid leukemia

(2010) H Andrikovics et al.   LEUKEMIA

The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival

(2010) A Scuto et al.   LEUKEMIA

Signal transducer and activator of transcription 3 activation up-regulates interleukin-6 autocrine production: a biochemical and genetic study of established cancer cell lines and clinical isolated human cancer cells

(2010) Wei-Lun Huang et al.   Molecular Cancer

Erythropoietin-Induced Activation of the JAK2/STAT5, PI3K/Akt, and Ras/ERK Pathways Promotes Malignant Cell Behavior in a Modified Breast Cancer Cell Line

(2010) Z. Shi et al.   MOLECULAR CANCER RESEARCH

AZ960, a Novel Jak2 Inhibitor, Induces Growth Arrest and Apoptosis in Adult T-Cell Leukemia Cells

(2010) J. Yang et al.   MOLECULAR CANCER THERAPEUTICS

Activity of the Aurora Kinase Inhibitor VX-680 against Bcr/Abl-Positive Acute Lymphoblastic Leukemias

(2010) F. Fei et al.   MOLECULAR CANCER THERAPEUTICS

Sorafenib Induces Growth Arrest and Apoptosis of Human Glioblastoma Cells through the Dephosphorylation of Signal Transducers and Activators of Transcription 3

(2010) Fan Yang et al.   MOLECULAR CANCER THERAPEUTICS

KRASmutant lung cancer cells are differentially responsive to MEK inhibitor due to AKT or STAT3 activation: Implication for combinatorial approach

(2010) Young-Kwang Yoon et al.   MOLECULAR CARCINOGENESIS

Safety and Efficacy of INCB018424, a JAK1 and JAK2 Inhibitor, in Myelofibrosis

(2010) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mechanism of MK-0457 efficacy against BCR–ABL positive leukemia cells

(2009) Seiichi Okabe et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Phase 2 study of CEP-701, an orally available JAK2 inhibitor, in patients with primary or post-polycythemia vera/essential thrombocythemia myelofibrosis

(2009) F. P. S. Santos et al.   BLOOD

Down syndrome acute lymphoblastic leukemia, a highly heterogeneous disease in which aberrant expression of CRLF2 is associated with mutated JAK2: a report from the International BFM Study Group

(2009) L. Hertzberg et al.   BLOOD

Benefits and harms of erythropoiesis-stimulating agents for anemia related to cancer: a meta-analysis

(2009) M. Tonelli et al.   CANADIAN MEDICAL ASSOCIATION JOURNAL

The JAK2 Inhibitor AZD1480 Potently Blocks Stat3 Signaling and Oncogenesis in Solid Tumors

(2009) Michael Hedvat et al.   CANCER CELL

Sustained Src Inhibition Results in Signal Transducer and Activator of Transcription 3 (STAT3) Activation and Cancer Cell Survival via Altered Janus-Activated Kinase-STAT3 Binding

(2009) B. Sen et al.   CANCER RESEARCH

Cucurbitacin B Induces Apoptosis by Inhibition of the JAK/STAT Pathway and Potentiates Antiproliferative Effects of Gemcitabine on Pancreatic Cancer Cells

(2009) N. H. Thoennissen et al.   CANCER RESEARCH

Recombinant human erythropoiesis-stimulating agents and mortality in patients with cancer: a meta-analysis of randomised trials

(2009) Julia Bohlius et al.   LANCET

CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients

(2009) A Pardanani et al.   LEUKEMIA

Recurrent numerical aberrations of JAK2 and deregulation of the JAK2-STAT cascade in lymphomas

(2009) Cecile Meier et al.   MODERN PATHOLOGY

Jak2 inhibitors: Rationale and role as therapeutic agents in hematologic malignancies

(2009) Jacqueline Sayyah et al.   Current Oncology Reports

Absence of JH2 domain mutation of the tyrosine kinase JAK2 in renal cell carcinomas

(2008) Jianming Zhao et al.   ACTA ONCOLOGICA

Stat3 Promotes Metastatic Progression of Prostate Cancer

(2008) Junaid Abdulghani et al.   AMERICAN JOURNAL OF PATHOLOGY

Vorinostat synergistically potentiates MK-0457 lethality in chronic myelogenous leukemia cells sensitive and resistant to imatinib mesylate

(2008) Y. Dai et al.   BLOOD

Cross talk of signals between EGFR and IL-6R through JAK2/STAT3 mediate epithelial–mesenchymal transition in ovarian carcinomas

(2008) M Colomiere et al.   BRITISH JOURNAL OF CANCER

Prevalence and clinical correlates ofJAK2mutations in Down syndrome acute lymphoblastic leukaemia

(2008) Amos Gaikwad et al.   BRITISH JOURNAL OF HAEMATOLOGY

A BCR-JAK2 fusion gene as the result of a t(9;22)(p24;q11) in a patient with acute myeloid leukemia

(2008) Gabriella Cirmena et al.   CANCER GENETICS AND CYTOGENETICS

Targeting Aurora Kinase with MK-0457 Inhibits Ovarian Cancer Growth

(2008) Y. G. Lin et al.   CLINICAL CANCER RESEARCH

Effects of the Aurora kinase inhibitor VX-680 on anaplastic thyroid cancer-derived cell lines

(2008) Y. Arlot-Bonnemains et al.   ENDOCRINE-RELATED CANCER

NovelSSBP2-JAK2fusion gene resulting from a t(5;9)(q14.1;p24.1) in pre-B acute lymphocytic leukemia

(2008) Jennifer L. Poitras et al.   GENES CHROMOSOMES & CANCER

Epidermal growth factor-induced ovarian carcinoma cell migration is associated with JAK2/STAT3 signals and changes in the abundance and localization of α6β1 integrin

(2008) Michelle Colomiere et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Jak2/Stat5 Signaling in Mammogenesis, Breast Cancer Initiation and Progression

(2008) Kay-Uwe Wagner et al.   JOURNAL OF MAMMARY GLAND BIOLOGY AND NEOPLASIA

Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome

(2008) Dani Bercovich et al.   LANCET

Multitargeted sequential therapy with MK-0457 and dasatinib followed by stem cell transplantation for T315I mutated chronic myeloid leukemia

(2008) Fermin M. Sanchez-Guijo et al.   LEUKEMIA RESEARCH

JAKs in pathology: Role of Janus kinases in hematopoietic malignancies and immunodeficiencies

(2008) William Vainchenker et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

SOCS regulation of the JAK/STAT signalling pathway

(2008) Ben A. Croker et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY