selective estrogen receptor degrader

Amcenestrant (SAR439859) is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).

Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).

Elacestrant S enantiomer is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant S enantiomer dihydrochloride is an low activity enantiomer of elacestrant dihydrochloride.

Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader .

Elacestrant dihydrochloride (DA-DKRAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader with IC50s of 48 for ERα and 870 nM for ERβ, respectively.

LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer.

ERα degrader10 is a potent, selective, orally active estrogen receptor α (ERα) degrader. It demonstrates strong ERα binding affinity (IC50 of 24.0 nM) and degradation capability (EC50 of 5.3 nM). This compound degrades ERα through a proteasome-mediated pathway and is utilized in breast cancer research.

ERα degrader11 (compound B16) is a selective estrogen receptor degrader designed for use as a probe in examining the ER status within ER-positive breast cancer cells.

ZN-c5 is a novel oral selective estrogen receptor degrader (SERD) with notable activity.

ER degrader 10 (Compound 51) is an orally active estrogen receptor (ER) selective degrader and antagonist, with a DC50 of 0.43 nM and an IC50 of 0.56 nM. It inhibits the proliferation of ER-positive cells, with an IC50 ranging from 0 to 15 nM. ER degrader 10 exhibits weak inhibitory activity on the hERG channel, with an IC50 greater than 40 μM. It has blood-brain barrier permeability, with a brain plasma ratio (Kp) of 3.05. In mouse models, ER degrader 10 demonstrates antitumor activity.

AZD9496 maleate is a highly potent and selective antagonist of the estrogen receptor alpha (ERα), exhibiting an IC50 value of 0.28 nM. This compound, AZD9496 maleate, is an orally bioavailable selective estrogen receptor degrader (SERD).

GNE-149 is an orally bioavailable compound and full antagonist of estrogen receptor α (ERα) with an IC50 of 0.053 nM, classified as a selective estrogen receptor degrader (SERD), holding potential for breast cancer research.

Rintodestrant (G1T48) is an orally active, non-steroidal, selective estrogen receptor degrader (SERD) and CDK4 6 inhibitor.

ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation. It can be used for the prevention and treatment of HER-positive breast cancer.

LX-039 is a potent, selective, orally active estrogen receptor degrader (EC50: 2.99 nM) with antitumor effects.LX-039 has indole C-3 chloride atoms.LX-039 has good pharmacokinetic properties in mice, low clearance, high blood levels and oral exposure.

Imlunestrant is a selective, orally active estrogen receptor degrader (SERD) that can be used in ER+ and HER2 breast cancer studies.

ERα degrader 5 is an orally active, selective estrogen receptor (ER) reducer that acts on ERα (EC50: 1.1 nM). ERα degrader 5 shows anti-tumour effects in vivo.

THIQ-40 is a novel potent erα antagonist and selective estrogen receptor degrader (serd), exhibiting good oral bioavailability, antitumor efficacy, and serd activity in vivo

Palazestrant (OP-1250) is an orally available and highly potent estrogen receptor antagonist and selective ER degrader with antitumor activity.Palazestrant inhibits 17b-estradiol (E2), inhibits MCF7 and CAMA-1 cell proliferation, and can be used in breast cancer research.

Imlunestrant tosylate (LY-3484356) is a potent, orally active selective estrogen receptor degrader (SERD) with purely antagonistic properties, effectively inhibiting estrogen receptor (ER)-dependent gene transcription and cell growth. This compound is applicable in research on ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) [1] [2].

Taragarestrant (D-0502) meglumine is a potent, orally active, and selective estrogen receptor degrader (SERD) demonstrating significant efficacy in ER+ breast cancer cell lines and xenograft models [1][2].

ER degrader 4, a selective and orally active compound, effectively degrades estrogen receptors and exhibits anti-tumor activity [1].

ER degrader 6 (compound 35s) is a potent selective estrogen receptor modulator (SERM) with the capacity to degrade Estrogen Receptor (ER)α. It disrupts the microtubule network, inhibits tubulin polymerization, and effectively suppresses tumor growth with minimal toxicity [1].