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IDH1057 is a novel, synthetic, small molecule inhibitor of heat shock protein 90 (Hsp90) developed by Ildong Pharmaceutical. It binds to the NH2-terminal ATP-binding pocket of Hsp90, exhibiting high binding affinity for the ATPase domain of Hsp90α. In preclinical studies, IDH1057 demonstrated potent anti-proliferative activity against various human tumor cell lines, including breast cancer (specifically triple-negative breast cancer), non-small cell lung cancer (NSCLC), and ovarian cancer. It has shown significant tumor growth inhibition in vivo in breast and ovarian cancer xenograft models when administered orally, with favorable pharmacokinetic and metabolic stability profiles.
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