CH5138303 is a potent and orally activeHsp90inhibitor. CH5138303 shows high binding affinity for N-terminalHsp90α, withK_dof 0.52 nM. CH5138303 shows potent anti-proliferative activity against humancancercell lines (HCT116 and NCI-N87), withIC₅₀values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastriccancerxenograft model^[1][2].

When used in combination with FLC, CH5138303 shows antifungal activitiy against azole-resistantC. albicans, with a FICI (fractional inhibitory concentration index) of 0.500^[2].

CH5138303 (SCID mice bearing NCI-N87 cells, 0-50 mg/kg, Orally, once daily for 11 days) shows potent antitumor efficacy with TGI (tumor growth inhibition) of 136% and a median effective dose (ED₅₀) of 3.9 mg/kg without significant loss of body weight^[1].

415.90

C₁₉H₁₈ClN₅O₂S

959763-06-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.