2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)-
![2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)- Structure](CAS/20210305/GIF/2407860-35-7.gif)
- CAS No.
- 2407860-35-7
- Chemical Name:
- 2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)-
- Synonyms
- ErSO;ErSo-DFP;(±)-ErSO;ErSO, 10 mM in DMSO;(R)-3-(4-hydroxyphenyl)-3-(4-(trifluoromethoxy)phenyl)-7-(trifluoromethyl)indolin-2-one;2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)-
- CBNumber:
- CB59803533
- Molecular Formula:
- C22H13F6NO3
- Molecular Weight:
- 453.33
- MDL Number:
- MOL File:
- 2407860-35-7.mol
2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)- Chemical Properties,Uses,Production
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
2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)- Preparation Products And Raw materials
Raw materials
Preparation Products
2H-Indol-2-one, 1,3-dihydro-3-(4-hydroxyphenyl)-3-[4-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)-, (3R)- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32376 | 58 |
| Chengdu DingDang Pharmaceutical Co., Ltd. | 028-86040038 13980902949; | market@dingdangchem.com | China | 1853 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24982 | 58 |
| Perseverant (Tianjin) Biomedical Technology Co., Ltd | 17777863707 | 17777863707@189.cn | China | 339 | 58 |
| Suzhou Haiben Pharmaceutical Co., Ltd | 19353112242 | 1816280386@qq.com | China | 8045 | 58 |
| Taizhou Chuanxu Pharmaceutical Technology Co., Ltd. | 13000000000 | 974144639@qq.com | China | 9344 | 58 |
| Sangon Biotech (Shanghai) Co.,Ltd. | 400-821-026 | Sales@sangon.com | China | 6710 | 58 |
| Cayman Chemical Company | 800-364-9897 | sales@caymanchem.com | China | 6838 | 58 |
| Aikon International Limited | 025-58851090 13408877820 | 2850281427@qq.com | China | 10000 | 58 |
