3-(2-Imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]benzamide
Title | Journal |
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Ponatinib efficacy and safety in Philadelphia chromosome-positive leukemia: final 5-year results of the phase 2 PACE trial. | Blood 20180726 |
Cytotoxicity of 34 FDA approved small-molecule kinase inhibitors in primary rat and human hepatocytes. | Toxicology letters 20180701 |
Mechanisms of mitochondrial toxicity of the kinase inhibitors ponatinib, regorafenib and sorafenib in human hepatic HepG2 cells. | Toxicology 20180215 |
Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance. | Journal of molecular biology 20170217 |
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. | Nature chemical biology 20151201 |
Efficacy of the polo-like kinase inhibitor rigosertib, alone or in combination with Abelson tyrosine kinase inhibitors, against break point cluster region-c-Abelson-positive leukemia cells. | Oncotarget 20150821 |
PF-114, a potent and selective inhibitor of native and mutated BCR/ABL is active against Philadelphia chromosome-positive (Ph+) leukemias harboring the T315I mutation. | Leukemia 20150501 |
A multi-parameter in vitro screen in human stem cell-derived cardiomyocytes identifies ponatinib-induced structural and functional cardiac toxicity. | Toxicological sciences : an official journal of the Society of Toxicology 20150101 |
BET protein antagonist JQ1 is synergistically lethal with FLT3 tyrosine kinase inhibitor (TKI) and overcomes resistance to FLT3-TKI in AML cells expressing FLT-ITD. | Molecular cancer therapeutics 20141001 |
Ponatinib is a potent inhibitor of wild-type and drug-resistant gatekeeper mutant RET kinase. | Molecular and cellular endocrinology 20130905 |
Identification of potent Yes1 kinase inhibitors using a library screening approach. | Bioorganic & medicinal chemistry letters 20130801 |
Ponatinib suppresses the development of myeloid and lymphoid malignancies associated with FGFR1 abnormalities. | Leukemia 20130101 |
Ponatinib as targeted therapy for FGFR1 fusions associated with the 8p11 myeloproliferative syndrome. | Haematologica 20130101 |
Philadelphia-positive acute lymphoblastic leukemia: current treatment options. | Current oncology reports 20121001 |
Platelet dysfunction associated with ponatinib, a new pan BCR-ABL inhibitor with efficacy for chronic myeloid leukemia resistant to multiple tyrosine kinase inhibitor therapy. | Haematologica 20120901 |
The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the MDR-associated ATP-binding cassette transporter ABCG2. | Molecular cancer therapeutics 20120901 |
Ponatinib is active against imatinib-resistant mutants of FIP1L1-PDGFRA and KIT, and against FGFR1-derived fusion kinases. | Leukemia 20120701 |
Clinical trials in chronic myeloid leukemia. | Current hematologic malignancy reports 20120601 |
Ponatinib may overcome resistance of FLT3-ITD harbouring additional point mutations, notably the previously refractory F691I mutation. | British journal of haematology 20120501 |
The ins and outs of bcr-abl inhibition. | Genes & cancer 20120501 |
Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models. | Molecular cancer therapeutics 20120301 |
The rise and fall of gatekeeper mutations? The BCR-ABL1 T315I paradigm. | Cancer 20120115 |
An in vitro screening to identify drug-resistant mutations for target-directed chemotherapeutic agents. | Methods in molecular biology (Clifton, N.J.) 20120101 |
The BCR-ABL35INS insertion/truncation mutant is kinase-inactive and does not contribute to tyrosine kinase inhibitor resistance in chronic myeloid leukemia. | Blood 20111110 |
[Is AP24534 (Ponatinib) the next treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia?]. | Bulletin du cancer 20110701 |
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. | Bioorganic & medicinal chemistry letters 20110615 |
New drugs for chronic myelogenous leukemia. | Current hematologic malignancy reports 20110601 |
Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. | Molecular cancer therapeutics 20110601 |
Philadelphia chromosome-positive acute lymphoblastic leukemia in childhood. | Korean journal of pediatrics 20110301 |
Targeting the BCR-ABL signaling pathway in therapy-resistant Philadelphia chromosome-positive leukemia. | Clinical cancer research : an official journal of the American Association for Cancer Research 20110115 |
Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance. | Chemical biology & drug design 20110101 |
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant. | Journal of medicinal chemistry 20100624 |
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. | Cancer cell 20091106 |
Inhibitors of ABL and the ABL-T315I mutation. | Current topics in medicinal chemistry 20080101 |