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
发现 3-[2-(咪唑并[1,2-b]哒嗪-3-基)乙炔基]-4-甲基-N-{4-[(4-甲基哌嗪-1-基)甲基]-3-(三氟甲基)苯基}苯甲酰胺 (AP24534),一种强效、口服活性的断点簇区域-abelson (BCR-ABL) 激酶泛抑制剂,包括 T315I 守门人突变体
期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/jm100395q
Wei-Sheng Huang, Chester A Metcalf, Raji Sundaramoorthi, Yihan Wang, Dong Zou, R Mathew Thomas, Xiaotian Zhu, Lisi Cai, David Wen, Shuangying Liu, Jan Romero, Jiwei Qi, Ingrid Chen, Geetha Banda, Scott P Lentini, Sasmita Das, Qihong Xu, Jeff Keats, Frank Wang, Scott Wardwell, Yaoyu Ning, Joseph T Sn