ChemicalBook CAS DataBase List 2407860-35-7

2407860-35-7

Name	2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)-
CAS	2407860-35-7
Molecular Formula	C22H13F6NO3
Molecular Weight	453.33
MOL File	2407860-35-7.mol

Chemical Properties

Boiling point	485.0±45.0 °C(Predicted)
density	1.461±0.06 g/cm3(Predicted)
solubility	DMSO: Soluble Methanol: Soluble
form	Solid
pka	9?+-.0.30(Predicted)
color	White to off-white

Hazard Information

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.

Animal Model:	Mice^[1]
Dosage:	0.5~40 mg/kg
Administration:	P.o.; 3 weeks
Result:	Sufficient for a robust response.

Animal Model:	Mice^[1]
Dosage:	40 mg/kg
Administration:	I.p.; 14 days
Result:	Metastatic burden was greatly reduced

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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