HSP(HSP90)抑制剂;HSP(HSP90) Inhibitors;;InformationCH5138303 CH5138303 is an orally available Hsp90 inhibitor with K d of 0.48 nM.TargetsHSP90α (Cell-free assay) 0.48 nM(Kd)In vitroCH5138303 shows high affinity to Hsp90αand potent cell growth inhibitory activity against an HCT116 colorectal cancer cell line and an NCI-N87 gastric cancer cell line with IC50 of 98 nM and 66 nM, respectively. [1] Besides, CH5138303 also demonstrates liver microsomal stability.In vivoCH5138303 (50 mg/kg p.o.) displays high oral bioavailability in mice and produces potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.Cell Research(from reference)Cell lines:HCT116 and NCI-N87 cell lines Concentrations:~10 μM Incubation Time:4 days