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2407860-35-7

2407860-35-7 structure
2407860-35-7 structure
  • Name: ErSO
  • Chemical Name: ErSO
  • CAS Number: 2407860-35-7
  • Molecular Formula: C22H13F6NO3
  • Molecular Weight: 453.33
  • Catalog: Research Areas Cancer
  • Create Date: 2021-09-10 18:49:33
  • Modify Date: 2025-08-25 15:05:43
  • 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].

Name ErSO
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].
Related Catalog
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]. 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]. 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.

Molecular Formula C22H13F6NO3
Molecular Weight 453.33
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