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DCC-2036

National Institutes of Health

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QuinolinesRebastinib Tosylate

Papers overview

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2019
2019
Imaging of Tie2 with a fluorescently labeled small molecule affinity ligand.
The receptor tyrosine kinase inhibitor, Tie2, has significant roles in endothelial signaling and angiogenesis, and is relevant in… 
2019
2019
An open label, multicenter, phase 1b/2 study of rebastinib (DCC-2036) in combination with carboplatin to assess safety, tolerability, and pharmacokinetics in patients with advanced or metastatic…
TPS2666 Background: Rebastinib is a potent, orally administered, kinase switch control inhibitor selectively targeting the tunica… 
2013
2013
Kinase Inhibitor Therapy in CML: It's What's Inside That Counts
The paradigm-shifting clinical success of imatinib in the treatment of chronic myeloid leukemia (CML) established continuous… 
2012
2012
Overcoming Gleevec-resistance by blocking oncogene addiction in malignant hematologic cells
In some types of tumors, malignant cells are highly dependent on the constitutive activation of a certain protein encoded by… 
2012
2012
Non-tyrosine kinase inhibitor-targeting of BCR–ABL expressing cells
Th e introduction in clinical practice of tyrosine kinase inhibitors (TKIs) targeting the oncogenic BCR – ABL protein has had a… 
Review
2011
Review
2011
Tyrosine kinase inhibitor therapy for chronic myeloid leukemia: approach to patients with treatment-naive or refractory chronic-phase disease.
The 21st century ushered in the dawn of a new era of targeted therapeutics and a dramatic shift in the management of chronic… 
2011
2011
A Phase 1 Study of DCC-2036, a Novel Oral Inhibitor of BCR-ABL Kinase, in Patients with Philadelphia Chromosome Positive (Ph+) Leukemias Including Patients with T315I Mutation
Abstract 601 Background. DCC-2036 is a novel and potent tyrosine kinase inhibitor (TKI) which binds to a novel region called the… 
2010
2010
A New BCR-ABL1 Mutation (L248R) Is Highly Resistant to Imatinib, Bosutinib, Nilotinib and Dasatinib, but Can Be Inhibited by AP-24534 and DCC-2036
Abstract 3398 Chronic Myeloid Leukemia (CML) treatment was radically modified by the discovery of imatinib (IM), a selective… 
Review
2010
Review
2010
Characteristics and Outcome of Chronic Myeloid Leukemia (CML) Patients with E255K and E255V BCR-ABL Kinase Domain Mutations.
Abstract 1226 Background: Mutations in the kinase domain (KD) of Abl represent the most common mechanism of resistance to… 
2007
2007
DCC-2036: A Novel Switch Pocket Inhibitor of ABL Tyrosine Kinase with Therapeutic Efficacy Against BCR-ABL T315I In Vitro and in a CML Mouse Model.
Therapy with ATP-competitive ABL kinase inhibitors, including imatinib (Gleevec), dasatinib (Sprycel), and nilotinib (Tasigna… 
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