Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805

F Baffert, CH Régnier, A De Pover… - Molecular cancer …, 2010 - AACR
The recent discovery of an acquired activating point mutation in JAK2, substituting valine at
amino acid position 617 for phenylalanine, has greatly improved our understanding of the …

Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F

L Ma, JR Clayton, RA Walgren, B Zhao, RJ Evans… - Blood cancer …, 2013 - nature.com
Owing to the prevalence of the JAK2V617F mutation in myeloproliferative neoplasms
(MPNs), its constitutive activity, and ability to recapitulate the MPN phenotype in mouse …

INCB018424, an Oral, Selective JAK2 Inhibitor, Shows Significant Clinical Activity in a Phase I/II Study in Patients with Primary Myelofibrosis (PMF) and Post …

S Verstovsek, H Kantarjian, A Pardanani, D Thomas… - 2007 - ashpublications.org
Background: A mutation in the Janus tyrosine kinase 2 gene (JAK2 V617F) has been
recognized in Philadelphia chromosome-negative myeloproliferative disorders, including PV …

WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation

S Verstovsek, T Manshouri, A Quintás-Cardama… - Clinical cancer …, 2008 - AACR
Purpose: The discovery of an activating somatic mutation in codon 617 of the gene encoding
the Janus kinase (JAK)-2 (JAK2 V617F) in patients with myeloproliferative disorders has …

JAK2 inhibitor therapy in myeloproliferative disorders: rationale, preclinical studies and ongoing clinical trials

A Pardanani - Leukemia, 2008 - nature.com
The recent identification of somatic mutations such as JAK2V617F that deregulate Janus
kinase (JAK)–signal transducer and activator of transcription signaling has spurred …

Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms

E Atallah, S Verstovsek - Expert review of anticancer therapy, 2009 - Taylor & Francis
The discovery of the Janus kinase (JAK) 2 V617F mutation in patients with myeloproliferative
neoplasms was a major milestone in understanding the biology of those disorders. Several …

[HTML][HTML] A phase I study of TG101348, an orally bioavailable JAK2-selective inhibitor, in patients with myelofibrosis

AD Pardanani, J Gotlib, C Jamieson, J Cortes… - Blood, 2008 - Elsevier
Background: The recent discovery of JAK2V617F, as an activating mutation in the majority of
patients with myeloproliferative neoplasms, has spurred development of JAK2-selective …

JAK2 mutants (eg, JAK2V617F) and their importance as drug targets in myeloproliferative neoplasms

K Gäbler, I Behrmann, C Haan - Jak-Stat, 2013 - Taylor & Francis
The Janus kinase 2 (JAK2) mutant V617F and other JAK mutants are found in patients with
myeloproliferative neoplasms and leukemias. Due to their involvement in neoplasia and …

Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms

A Quintás-Cardama, K Vaddi, P Liu… - Blood, The Journal …, 2010 - ashpublications.org
Constitutive JAK2 activation in hematopoietic cells by the JAK2V617F mutation recapitulates
myeloproliferative neoplasm (MPN) phenotypes in mice, establishing JAK2 inhibition as a …

Discovery and preclinical characterization of INCB018424, a selective JAK2 inhibitor for the treatment of myeloproliferative disorders.

J Fridman, R Nussenzveig, P Liu, J Rodgers, T Burn… - 2007 - ashpublications.org
Activating mutations in Janus kinase 2 (JAK2) have recently been identified in the majority of
Philadelphia chromosome negative (Ph-) myeloproliferative disorders (MPDs). Importantly …