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estrogen receptor positive breast cancer

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Estrogen Receptor/ERR (15) Akt (1) Amino Acid Derivatives (1) Androgen Receptor (2) Apoptosis (4) Autophagy (1) Carboxypeptidase (1) Cytochrome P450 (1) EGFR (1) HDAC (1) Isotope-Labeled Compounds (1) LDLR (1) mTOR (1) PROTACs (2) Sodium Channel (1) Steroid Sulfatase (1) TRP Channel (1) VD/VDR (1)
By Research Areas:	Cancer (25) Inflammation/Immunology (1) Metabolic Disease (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Targets Recommended: BCRP Estrogen Receptor/ERR BRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-138642

Vepdegestrant Maximum Cited Publications 6 Publications Verification ARV-471	PROTACs Estrogen Receptor/ERR	Cancer
Vepdegestrant (ARV-471) is an orally active PROTAC **estrogen receptor** degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC₅₀) of about 2 nM .

HY-145572

Imlunestrant 1 Publications Verification LY-3484356	Estrogen Receptor/ERR	Cancer
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) .

HY-W142080

α-Methyl-DL-tryptophan α-Methyltryptophan	mTOR Autophagy Apoptosis Amino Acid Derivatives	Metabolic Disease Cancer
α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .

HY-145572A

Imlunestrant tosylate 1 Publications Verification LY-3484356 tosylate	Estrogen Receptor/ERR	Cancer
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) .

HY-153468

ErSO-TFPy TEQ103; Sera2	Sodium Channel TRP Channel	Cancer
ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer .

HY-112596

H3B-6545 3 Publications Verification	Estrogen Receptor/ERR	Cancer
H3B-6545 is an oral, selective **estrogen receptor covalent antagonist (SERCA*) for the research of metastatic ER-positive, HER2-negative breast* cancer .

HY-177760

PrCP-7414	Carboxypeptidase Apoptosis Akt	Cancer
PrCP-7414 is a prolyl carboxypeptidase (PRCP) inhibitor. PrCP-7414 blocks PRCP-mediated activation of the IGF1R/HER3 signaling pathway and subsequent AKT activation. PrCP-7414 exhibits pro-apoptotic, anti-tumor and synergistic cytotoxic activities, and inhibits the proliferation and survival of triple-negative breast cancer cells. PrCP-7414 can be used for the research of breast cancer .

HY-112596A

H3B-6545 hydrochloride 3 Publications Verification	Estrogen Receptor/ERR	Cancer
H3B-6545 hydrochloride is an oral, selective **estrogen receptor covalent antagonist (SERCA*) for the research of metastatic ER-positive, HER2-negative breast* cancer .

HY-159613

PELP1-IN-1	Apoptosis Estrogen Receptor/ERR	Inflammation/Immunology Cancer
PELP1-IN-1 is a PELP1 inhibitor and an apoptosis inducer with no cytotoxic activity against non-cancer cell lines. PELP1-IN-1 targets wild-type, mutant and drug-resistant ER ⁺ breast cancer, and promotes PELP1 degradation through the proteasome pathway. As an analog of SMIP34 (HY-169903), PELP1-IN-1 is applicable to the research of estrogen receptor α-positive breast cancer .

HY-138642S

Vepdegestrant-d5 ARV-471-d₅	Isotope-Labeled Compounds	Cancer
Vepdegestrant-d₅ (ARV-471-d₅) is the deuterium labeled Vepdegestrant (HY-138642). Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a DC₅₀ of about 2 nM .

HY-123868

KW-2581	Steroid Sulfatase	Cancer
KW-2581 is a steroidal selective steroid sulfatase (STS) inhibitor with an IC₅₀ of 4 nM. KW-2581 inhibits STS activity of ZR-75-1 cells with an IC₅₀ of 13 nM. KW-2581 inhibits the E1S-stimulated growth of ZR-75-1 cells with an IC₅₀ of 0.18 nM. KW-2581 inhibits sulfated-estrogen dependent growth of breast cancer cells both in vitro and in vivo. KW-2581 induced regression in E1S-induced tumor growth. KW-2581 can be studied in research on hormone receptors-positive breast cancer .

HY-138642A

(Rac)-Vepdegestrant (Rac)-ARV-471	Estrogen Receptor/ERR PROTACs	Cancer
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC **estrogen receptor** degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC₅₀) of about 2 nM .

HY-107550

NCT-14b	HDAC	Cancer
NCT-14b is a HDAC6-selective inhibitor. NCT-14b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells .

HY-174231

EGFR-IN-163	EGFR Apoptosis	Cancer
EGFR-IN-163 (Compound 13) is a competitive epidermal growth factor receptor (EGFR) inhibitor (IC₅₀=0.079 μM, selective for HER-2 inhibition). EGFR-IN-163 induces tumor cell apoptosis and cell cycle arrest at G₂/M phase. EGFR-IN-163 is promising for research of estrogen receptor-positive (ER+) breast cancer .

HY-106839

NKS-01	Estrogen Receptor/ERR	Metabolic Disease Cancer
NKS-01 is a selective **estrogen receptor** modulator. NKS-01 can be used for the research of cancer, such as estrogen receptor-positive breast cancer .

HY-171477

Metahexestrol	Estrogen Receptor/ERR	Cancer
Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED₅₀ = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .

HY-178463

F0840-0093	Estrogen Receptor/ERR	Cancer
F0840-0093 is a highly selective estrogen receptor α (ERα) degrader. F0840-0093 exhibits potent antiproliferative activity against T47D cells with an IC₅₀ value of 4.65 μM. F0840-0093 is promising for research of estrogen receptor-positive (ER+) breast cancer .

HY-124403

D 15413	Estrogen Receptor/ERR	Cancer
D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 ^-7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .

HY-163947

UG-480	VD/VDR	Cancer
UG-480 is a gemini analog that effectively stabilizes the active VDR conformation. UG-480 has antiproliferative effects in estrogen receptor-positive MCF-7 breast adenocarcinoma cells. UG-480 can be used in cancer research .

HY-138089

17β-Hydroxy exemestane	Androgen Receptor Estrogen Receptor/ERR LDLR	Metabolic Disease Cancer
17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC₅₀ = 69 nM) and an androgen receptor (AR) agonist (IC₅₀ = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC₅₀ = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC₅₀= 2.7 μM) and T47D breast cancer cells (EC₅₀s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats .

HY-180535

Aromatase-IN-8	Cytochrome P450	Cancer
Aromatase-IN-8 is a selective Aromatase inhibitor against an IC₅₀ of 0.05 µM. Aromatase-IN-8 exhibits selective antiproliferative effects against estrogen receptor-positive breast cancer cell lines, while showing no toxicity toward non-tumoral cells. Aromatase-IN-8 suppresses estrogen active, increases testosterone levels, and downregulates estrogen receptor expression and phosphorylation. Aromatase-IN-8 can be used for triple negative breast cancer research .

HY-168101

ERα degrader 11	Estrogen Receptor/ERR	Cancer
ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells .

HY-176956

ER degrader 13	Estrogen Receptor/ERR	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 .

HY-182722

UT-105	Androgen Receptor	Cancer
UT-105 is an orally active androgen receptor (AR) degrader. UT-105 binds to the N-terminal domain of AR and promotes its degradation. UT-105 inhibits the growth of enzalutamide-resistant breast cancer xenografts and reduces tumor cell proliferation. UT-105 can be used in the research of estrogen receptor-positive breast cancer .

HY-124627

THIQ 40	Estrogen Receptor/ERR	Cancer
THIQ-40 is a tetrahydroisoquinoline-based, orally active, and selective **estrogen receptor ERα degrader (SERD) (IC₅₀*=17 nM), with antitumor efficacy. THIQ-40 possesses functional ERα antagonistic activity, promotes ERα degradation and forms stable ERαLBD complexes. THIQ-40 shows the characteristic of rapid racemization in multi-species plasma. THIQ-40 can be widely applied to studies on the relevant mechanisms and drug development of ERα-positive* breast cancer .

Cat. No.	Product Name

HY-L074

Anti-Breast Cancer Compound Library	3,232 compounds
Breast cancer is the most frequent cancer among women, impacting 2.1 million women each year, and also causes the greatest number of cancer-related deaths among women. Surgery is usually the first type of treatment for breast cancer, which is usually followed by chemotherapy or radiotherapy or, in some cases, hormone or targeted therapies, especially for metastatic breast cancer (MBC). Breast cancer is a heterogeneous disease, which is categorized into 3 major subtypes based on the presence or absence of molecular markers for estrogen or progesterone receptors and human epidermal growth factor 2 (ERBB2; formerly HER2): hormone receptor positive/ERBB2 negative (70% of patients), ERBB2 positive (15%-20%), and triple-negative (tumors lacking all 3 standard molecular markers; 15%). Different intrinsic subtypes exhibit different tumor behavior with different prognoses, and may require specific targeted therapies to maximize treatment effectiveness. Otherwise, some signaling pathways also play important roles in the development of breast cancer, such as NF-κB Signaling Pathway, TGF-beta Signaling Pathway, PI3K/AKT/mTOR signaling pathway and Notch Signaling Pathway. These signaling pathways offer ideal targets for development of new targeted therapies for breast cancer. MCE supplies a unique collection of 3,232 compounds with identified and potential anti-breast cancer activity. MCE Anti-Breast Cancer Compound Library is a useful tool for anti-breast cancer drugs screening.

Anti-Breast Cancer Compound Library

3,232 compounds

Breast cancer is the most frequent cancer among women, impacting 2.1 million women each year, and also causes the greatest number of cancer-related deaths among women. Surgery is usually the first type of treatment for breast cancer, which is usually followed by chemotherapy or radiotherapy or, in some cases, hormone or targeted therapies, especially for metastatic breast cancer (MBC).

Breast cancer is a heterogeneous disease, which is categorized into 3 major subtypes based on the presence or absence of molecular markers for estrogen or progesterone receptors and human epidermal growth factor 2 (ERBB2; formerly HER2): hormone receptor positive/ERBB2 negative (70% of patients), ERBB2 positive (15%-20%), and triple-negative (tumors lacking all 3 standard molecular markers; 15%). Different intrinsic subtypes exhibit different tumor behavior with different prognoses, and may require specific targeted therapies to maximize treatment effectiveness. Otherwise, some signaling pathways also play important roles in the development of breast cancer, such as NF-κB Signaling Pathway, TGF-beta Signaling Pathway, PI3K/AKT/mTOR signaling pathway and Notch Signaling Pathway. These signaling pathways offer ideal targets for development of new targeted therapies for breast cancer.

MCE supplies a unique collection of 3,232 compounds with identified and potential anti-breast cancer activity. MCE Anti-Breast Cancer Compound Library is a useful tool for anti-breast cancer drugs screening.

Cat. No.	Product Name	Target	Research Area

HY-W142080

α-Methyl-DL-tryptophan α-Methyltryptophan	mTOR Autophagy Apoptosis Amino Acid Derivatives	Metabolic Disease Cancer
α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .

Cat. No.	Product Name	Chemical Structure

HY-138642S

Vepdegestrant-d5
Vepdegestrant-d₅ (ARV-471-d₅) is the deuterium labeled Vepdegestrant (HY-138642). Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a DC₅₀ of about 2 nM .

Vepdegestrant-d5

Vepdegestrant-d₅ (ARV-471-d₅) is the deuterium labeled Vepdegestrant (HY-138642). Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a DC₅₀ of about 2 nM .

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