HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance

MeSH terms

• Aminopyridines
• Animals
• Antineoplastic Agents / pharmacology*
• Apoptosis / drug effects
• Benzamides
• Blotting, Western
• Cell Proliferation / drug effects
• Drug Resistance, Neoplasm / drug effects*
• Fusion Proteins, bcr-abl / antagonists & inhibitors*
• Fusion Proteins, bcr-abl / genetics
• Fusion Proteins, bcr-abl / metabolism
• Humans
• Imatinib Mesylate
• Leukemia, Experimental / drug therapy
• Leukemia, Experimental / metabolism
• Leukemia, Experimental / pathology
• Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy*
• Leukemia, Myelogenous, Chronic, BCR-ABL Positive / metabolism
• Leukemia, Myelogenous, Chronic, BCR-ABL Positive / pathology
• Mice
• Mice, Nude
• Phosphorylation / drug effects
• Piperazines / pharmacology*
• Protein Kinase Inhibitors / pharmacology*
• Proto-Oncogene Proteins c-kit / metabolism
• Pyridines / pharmacology*
• Pyrimidines / pharmacology*
• RNA, Messenger / genetics
• Receptor, Platelet-Derived Growth Factor beta / metabolism
• Reverse Transcriptase Polymerase Chain Reaction
• Survival Rate
• Tumor Cells, Cultured
• Xenograft Model Antitumor Assays