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

RM Stone, DJ DeAngelo, V Klimek, I Galinsky, E Estey… - Blood, 2005 - ashpublications.org
Leukemic cells from 30% of patients with acute myeloid leukemia (AML) have an activating
mutation in the FLT3 (fms-like tyrosine kinase) gene, which represents a target for drug …

FLT3 mutations: biology and treatment

D Small - ASH Education Program Book, 2006 - ashpublications.org
FLT3 is a receptor tyrosine kinase with important roles in hematopoietic stem/progenitor cell
survival and proliferation. It is mutated in about 1/3 of acute myeloid leukemia (AML) …

Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia

BD Smith, M Levis, M Beran, F Giles, H Kantarjian… - Blood, 2004 - ashpublications.org
Activating mutations of FMS-like tyrosine kinase 3 (FLT3) are present in approximately 30%
of patients with de novo acute myeloid leukemia (AML) and are associated with lower cure …

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

F Heidel, FK Solem, F Breitenbuecher, DB Lipka… - Blood, 2006 - ashpublications.org
Activating mutations in the FLT3 tyrosine kinase (TK) occur in approximately 35% of patients
with acute myeloid leukemia (AML). Therefore, targeting mutated FLT3 is an attractive …

Identification of a novel activating mutation (Y842C) within the activation loop of FLT3 in patients with acute myeloid leukemia (AML)

T Kindler, F Breitenbuecher, S Kasper, E Estey, F Giles… - Blood, 2005 - ashpublications.org
Fms-like tyrosine kinase 3 (FLT3) receptor mutations as internal tandem duplication (ITD) or
within the kinase domain are detected in up to 35% of patients with acute myeloid leukemia …

A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response

KW Pratz, J Cortes, GJ Roboz, N Rao… - Blood, The Journal …, 2009 - ashpublications.org
Internal tandem duplication mutations of FLT3 (FLT3/ITD mutations) are common in acute
myeloid leukemia (AML) and confer a poor prognosis. This would suggest that FLT3 is an …

A FLT3 tyrosine kinase inhibitor is selectively cytotoxic to acute myeloid leukemia blasts harboring FLT3 internal tandem duplication mutations

M Levis, KF Tse, BD Smith, E Garrett… - Blood, The Journal of …, 2001 - ashpublications.org
Internal tandem duplication (ITD) mutations of the receptor tyrosine kinase FLT3 have been
found in 20% to 30% of patients with acute myeloid leukemia (AML). These mutations …

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

J Cools, N Mentens, P Furet, D Fabbro, JJ Clark… - Cancer research, 2004 - AACR
Mutations in the receptor tyrosine kinase FLT3 occur frequently in patients with acute
myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). Small molecules that …

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 …

S Knapper, KI Mills, AF Gilkes, SJ Austin, V Walsh… - Blood, 2006 - ashpublications.org
The receptor tyrosine kinase FLT3 is a promising molecular therapeutic target in acute
myeloid leukemia (AML). Activating mutations of FLT3 are present in approximately one …

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

E Weisberg, C Boulton, LM Kelly, P Manley, D Fabbro… - Cancer cell, 2002 - cell.com
Constitutively activating FLT3 receptor mutations have been found in 35% of patients with
acute myeloblastic leukemia (AML). Here we report the identification of a small molecule …