Estrogen Receptor/ERR Degrader

Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC).

Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC).

ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC₅₀ values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity.

LSZ-102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with an IC₅₀ value of 0.2 nM.

UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC₅₀ values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.

Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models.

GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC₅₀ value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC₅₀=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.

GDC-0927 Racemate (SRN-927 Racemate) is an estrogen receptor (ER) degrader that can effectively inhibit the activity of ER-α with an IC₅₀ value of 0.2 nM and can be used in diseases related to estrogen receptors.

Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models.

ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC₅₀ = 0.3 nM) and binds with high affinity to ERα and ERβ (IC₅₀ = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer.

ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC₅₀ value of 0.15 μM.

OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders.

ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model.

Elacestrant-d₁₀ is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC₅₀s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER⁺ breast cancer cell lines in vitro and in vivo.

PROTAC ERα Degrader-8 (compound ii-56) is a potent PROTAC degrader of Erα, with DC₅₀ of 0.000006 μM in MCF7 cells.

PROTAC ER Degrader-15 (Compound 40) is an orally active degrader of the estrogen receptor (ER) with anticancer activity，which can be used in breast cancer research (Pink: Target Protein Ligand (HY-170334); Black: Linker (HY-30756); Blue: E3 Ligase Ligand (HY-138793); E3 Ligase Ligand-Linker Conjugate (HY-169979)).

ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC₅₀ of 0.43 nM and an IC₅₀ of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC₅₀s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC₅₀ >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model.

PROTAC ER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader (DC₅₀: <10 nM), and inhibits MCF-7 proliferation (DC₅₀: <10 nM). PROTAC ER Degrader-12 has anticancer effect.

ER degrader 7 is an estrogen receptor α (ERα) degrader and a tubulin (tubulin) inhibitor. ER degrader 7 inhibits the cell viability of various cancer cell lines. ER degrader 7 disrupts the microtubule network in breast cancer cells, induces G2/M phase cell cycle arrest, and exhibits concentration-dependent accumulation in Tamoxifen-resistant LCC2 cells. ER degrader 7 suppresses tumor growth in vivo without causing body weight loss. ER degrader 7 can be applied in studies related to breast cancer.

ER degrader 13 (Compound 37) is an estrogen receptor (ER) degrader. ER degrader 13 has a significant inhibitory effect on the proliferation of ER-positive breast cancer MCF-7 cells.