| Identification | Back Directory | [Name]
2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)- | [CAS]
2407860-35-7 | [Synonyms]
ErSO
ErSo-DFP
2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)- | [Molecular Formula]
C22H13F6NO3 | [MOL File]
2407860-35-7.mol | [Molecular Weight]
453.33 |
| Chemical Properties | Back Directory | [Boiling point ]
485.0±45.0 °C(Predicted) | [density ]
1.461±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
9?+-.0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
ErSO is an activator of the unfolded protein response which eradicates human breast tumors in mice. ErSO activates the anticipatory unfolded protein response (a-UPR) and induces rapid and selective necrosis of ERα-positive breast cancer cell lines in vitro. In multiple orthotopic models, ErSO treatment given either orally or intraperitoneally for 14 to 21 days induced tumor regression without recurrence. In a cell line tail vein metastasis model, ErSO was also effective at inducing regression of most lung, bone, and liver metastases. ErSO treatment induced almost complete regression of brain metastases in mice carrying intracranial human breast cancer cell line xenografts. | [Uses]
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer[1]. | [in vivo]
ErSO (10 or 40 mg/kg; p.o.; 21 days) results in elimination of these tumors, with >90% reduction in all cases[1].
ErSO (0.5~40 mg/kg; p.o.; 3 weeks) is sufficient for a robust response[1].
ErSO (10 and 40 mg/kg; p.o.; 14 days) induces >10,000-fold regression of TYS-luciferase-expressing breast tumors in all five mice and >100,000-fold regression (to undetectable amounts) within 14 days as shown by bioluminescent imaging of luciferase as compared to vehicle-treated mice[1].
ErSO (40 mg/kg; i.p.; 14 days) greatly reduces metastatic burden[1].
ErSO treatment ablates mutant ERα breast cancer cell line xenografts and a PDX mouse model[1]. | Animal Model: | Nu/J mice[1] | | Dosage: | 10 or 40 mg/kg | | Administration: | P.o.; 21 days | | Result: | Resulted in elimination of these tumors, with >90% reduction in all cases.
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| Animal Model: | Mice[1] | | Dosage: | 0.5~40 mg/kg | | Administration: | P.o.; 3 weeks | | Result: | Sufficient for a robust response.
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| Animal Model: | Mice[1] | | Dosage: | 40 mg/kg | | Administration: | I.p.; 14 days | | Result: | Metastatic burden was greatly reduced
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| [References]
[1] Boudreau MW, et al. A small-molecule activator of the unfolded protein response eradicates human breast tumors in mice. Sci Transl Med. 2021;13(603):eabf1383. DOI:10.1126/scitranslmed.abf1383 |
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