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ErSO 

Cat. No.: HY-132247
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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.

For research use only. We do not sell to patients.

ErSO Chemical Structure

ErSO Chemical Structure

CAS No. : 2407860-35-7

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Description

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].

IC50 & Target

a-UPR[1]

In Vitro

ErSO (1~1000 nM; 24 hours; MCF-7 cells) shows that IC50 value is 20.3 nM in MCF-7 cells and inhibits cell viability[1].
ErSO (1 μM; 24 hours; TYS cells) rapidly kills ERα-positive breast cancer cells. ErSO is effective against both the breast cancer cell lines expressing wild-type ERα and the ERαY537S and ERαD538G mutations such as human breast cancer cell lines TYS and TDG. ErSO is also effective against tamoxifen- and fulvestrant-resistant breast cancer cell lines containing wild-type ERα. ErSO activity is independent of the presence of estrogen. ErSO induces rapid killing of ERα-positive MCF-7 human breast cancer cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 1~1000 nM
Incubation Time: 24 hours
Result: Showed that IC50 value is 20.3 nM in MCF-7 cells and inhibited cell viability.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

453.33

Formula

C₂₂H₁₃F₆NO₃

CAS No.
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Storage

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ErSO
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