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Chemical Structure : ErSO
Catalog No.: PC-72844Not For Human Use, Lab Use Only.
ErSO is a small molecule activator of the unfolded protein response (UPR), activates the a-UPR, induces rapid and selective necrosis of ERα-positive breast cancer cell lines in vitro.
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ErSO is a small molecule activator of unfolded protein response (UPR), activates the a-UPR, induces rapid and selective necrosis of ERα-positive breast cancer cell lines in vitro.
ErSO inhibits cell viability of breast cancer cell lines expressing wild-type ERα and the ERαY537S and ERαD538G mutations with IC50 of 11-43 nM (TYS and TDG).
ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR.
ErSO does not compete with estrogens for binding to ERα and selectively kills ERα-positive breast cancer cells including those harboring known resistance-mediating ERα mutations.
ErSO kills ERα-positive breast cancer cell lines in vitro induces complete regression in orthotopic cell line xenograft and patient-derived xenograft (PDX) mouse models, regardless of ERα mutational status and without recurrence after cessation of treatment.
ErSO causes complete regression of most tumors in a fulvestrant-resistant, ERα-mutant, PDX mouse model andmetastatic breast cancer mouse models.
| M.Wt | 453.34 | |
| Formula | C22H13F6NO3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Boudreau MW, et al. Sci Transl Med. 2021 Jul 21;13(603):eabf1383.
2. Boudreau MW, et al. J Med Chem. 2022 Mar 10;65(5):3894-3912.
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