Name | ch5138303 |
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Description | CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values 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 gastric cancer xenograft model[1][2]. |
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Related Catalog | |
Target |
HSP90α:0.52 nM (Kd) |
In Vitro | When used in combination with FLC, CH5138303 shows antifungal activitiy against azole-resistant C. albicans, with a FICI (fractional inhibitory concentration index) of 0.500[2]. |
In Vivo | 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]. |
References |
Molecular Formula | C19H18ClN5O2S |
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Molecular Weight | 415.89700 |
Exact Mass | 415.08700 |
PSA | 142.31000 |
LogP | 4.59670 |
Storage condition | -20℃ |