ErSO | UPR activator | Probechem Biochemicals

Chemical Structure : ErSO

CAS No.: 2407860-35-7

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ErSO (UPR activator)

货号: 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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5 mg	￥2280	In stock
10 mg	￥3780	In stock
25 mg	￥5780	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	453.34
分子式	C22H13F6NO3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-3-(4-hydroxyphenyl)-3-(4-(trifluoromethoxy)phenyl)-7-(trifluoromethyl)indolin-2-one

参考文献

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.

ErSO (UPR activator)

生物&药学活性

物理化学性质&存储条件

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ErSO (UPR activator)

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