| 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 |
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| Target |
HSP90α:0.52 nM (Kd)
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| 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].
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| 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].
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| References |
[1]. Atsushi Suda, et al. Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors. Bioorganic & Medicinal Chemistry. 15 January 2014;22(2):892-905. [2]. Yuan R, et al. Effects of Hsp90 Inhibitor Ganetespib on Inhibition of Azole-Resistant Candida albicans. Front Microbiol. 2021 May 20;12:680382.
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