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].

PROTAC ERα Degrader-11 (Compound W2) (96 h) exhibits excellent cell inhibitory activity with IC₅₀ values of 0.19 μM (MCF-7), 1.40 μM (MCF-7EGFR), 4.31 μM (MCF-7D538G) and 9.29 μM (MCF-7Y537S)^[1].

PROTAC ERα Degrader-11 (10 μM, 0-24 h) degrades ERα in MCF-7 cells in a time-dependent manner within 24 h, which is reduced after the addition of the ERα ligand (OBHSA) (HY-167701) or CRBN ligand^[1].

PROTAC ERα Degrader-11 (0.5-10 μM, 24 h) does not degrade ERβ in PC9 cells^[1].

PROTAC ERα Degrader-11 (0-80 μM, 10-360 min) exhibits a concentration-dependent and time-dependent proportional increase in fluorescence intensity^[1].

PROTAC ERα Degrader-11 (1-20 μM, 48 h) induces G2/M phase arrest and induces apoptosis in MCF-7 cells^[1].

PROTAC ERα Degrader-11 (10 μM, 0-60 min) exhibits high photostability in the presence of ERα^[1].

PROTAC ERα Degrader-11 (0.1-20 μM) does not induce significant damage to the blood cell membranes in SD rats^[1].

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

PROTAC ERα Degrader-11 (Compound W2) (500 mg/kg, i.p. single dose) is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice^[1].

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

997.00

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]