WXFL1024H251

WXFL1024H251 is a novel, second-generation small-molecule heat shock protein 90 (Hsp90) inhibitor developed by WuXi AppTec and Chia Tai Tianqing. Unlike first-generation Hsp90 inhibitors of the ansamycin family, WXFL1024H251 features a distinct chemical structure. In preclinical studies, it demonstrated potent anti-proliferative activity against various cancer cell lines, including A549 (KRAS-mutant lung cancer) and BT474 (ER+ and ERBB2+ breast cancer). In vivo, intravenous administration of WXFL1024H251 showed significant anti-tumor efficacy in BT474 breast cancer xenograft models, which was associated with client protein maturation and HSP70 up-regulation.