PROTAC ERα Degrader-11

PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer. (Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880) ) [1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Estrogen Receptor/ERR; Fluorescent Dye; PROTACs

Related Pathways

Apoptosis; Others; PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=S(N(C1=CC=C(OCC(NCCCCCCOC2=CC3=CC=CC(C4=O)=C3C(C(N4C(C5=O)CCC(N5)=O)=O)=C2)=O)C=C1)CC(F)(F)F)([C@H]6[C@@H]7C(C8=CC=C(O)C=C8)=C(C9=CC=C(O)C=C9)[C@@H](O7)C6)=O

Molecular Formula

C51H47F3N4O12S

Molecular Weight

997.00

References & Citations

[1]Wu Y, et al. Discovery of ERα-targeting PROTACs with intrinsic fluorescence for precision theranostics of breast cancer. RSC Med Chem. 2025 May 22.