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ErSO

CAS No. : 2407860-35-7

MCE 站：ErSO

产品活性：ErSO是一种选择性预期折叠蛋白反应 (a-UPR) 激活剂。ErSO 通过 ERα 诱导 a-UPR 产生强而持久的细胞毒性。ErSO 可用于癌症研究。

研究领域：Others

作用靶点：Others

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.
ErSO (1 μM; 24 hours; TYS cells) rapidly killed 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 was 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.

In Vivo: ErSO (10 or 40 mg/kg; p.o.; 21 days) results in elimination of these tumors, with >90% reduction in all cases.
ErSO (0.5~40 mg/kg; p.o.; 3 weeks) is sufficient for a robust response.
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.
ErSO (40 mg/kg; i.p.; 14 days) greatly reduces metastatic burden.
ErSO treatment ablates mutant ERα breast cancer cell line xenografts ａnd a PDX mouse model.

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