| Identification | Back Directory | [Name]
2H-Indol-2-one, 3-(4,4-difluoro-1-piperidinyl)-1,3-dihydro-3-(4-hydroxyphenyl)-7-(trifluoromethyl)- | [CAS]
2768139-73-5 | [Synonyms]
(Rac)-ErSO-DFP
2H-Indol-2-one, 3-(4,4-difluoro-1-piperidinyl)-1,3-dihydro-3-(4-hydroxyphenyl)-7-(trifluoromethyl)- | [Molecular Formula]
C20H17F5N2O2 | [MOL File]
2768139-73-5.mol | [Molecular Weight]
412.35 |
| Hazard Information | Back Directory | [Uses]
(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1)[1]. | [in vivo]
(Rac)-ErSO-DFP (compound 2) (5 mg/kg; i.v.; 3xq.wk.) shows a sustained activity of againsting ERα+ breast cancer at low doses[1]. | Animal Model: | Ovariectomized Nu/J mice (MCF-7 orthotopic tumor model)[1]. | | Dosage: | 5 mg/kg | | Administration: | Intravenous injection; once-a-week for 3 total doses. | | Result: | Maintained the ability to regress MCF-7 tumors in a mouse model of ERα+ breast cancer. |
| [References]
[1] Hergenrother, et al. Enzyme-activating compounds and compositions. Patent WO2022087234A1. |
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