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breast cancer with ER

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-138642
    Vepdegestrant
    5+ Cited Publications

    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 .
    Vepdegestrant
  • HY-19822
    Elacestrant
    Maximum Cited Publications
    17 Publications Verification

    RAD1901

    Estrogen Receptor/ERR Cancer
    Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
    Elacestrant
  • 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) .
    Imlunestrant
  • HY-136255
    Camizestrant
    5+ Cited Publications

    AZD-9833

    Estrogen Receptor/ERR Cancer
    Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER + HER2-advanced breast cancer .
    Camizestrant
  • HY-153444

    PF-07248144

    Histone Acetyltransferase Cancer
    Prifetrastat (PF-07248144), a first-in-class, selective, and orally active KAT6A and KAT6AB inhibitor. Prifetrastat can be used for the study of ER+/HER2− breast cancer .
    Prifetrastat
  • 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) .
    Imlunestrant tosylate
  • HY-B0412
    Estriol
    5 Publications Verification

    Oestriol

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .
    Estriol
  • HY-19822A
    Elacestrant dihydrochloride
    Maximum Cited Publications
    17 Publications Verification

    RAD1901 dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
    Elacestrant dihydrochloride
  • HY-153468

    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 .
    ErSO-TFPy
  • HY-133017
    Amcenestrant
    3 Publications Verification

    SAR439859

    Estrogen Receptor/ERR Cancer
    SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER + breast cancer.
    Amcenestrant
  • 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 .
    H3B-6545
  • HY-12825

    Estrogen Receptor/ERR Phospholipase Cancer
    BHPI is a nuclear receptor ERα inhibitor. BHPI activates PLCγ and UPR. BHPI has antitumor activity against breast, endometrial, and ovarian cancers .
    BHPI
  • HY-50767S

    PD 0332991-d8

    Isotope-Labeled Compounds CDK Cancer
    Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .
    Palbociclib-d8
  • HY-103457

    Estrogen Receptor/ERR Cancer
    Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
    Y134
  • HY-N1180

    SARS-CoV Keap1-Nrf2 Infection
    Tanshinlactone is a compound found in Salvia miltiorrhiza with anti-coronavirus (CoV) and anti-tumor activities. Tanshinlactone induces methuocytic cell death (methuosis) by activating the NRF2 pathway, and selectively kills ER +, HER2 +/EGFR + breast cancer cells. Tanshinlactone is applicable to research related to breast cancer and coronavirus infections .
    Tanshinlactone
  • HY-149480

    PROTACs Estrogen Receptor/ERR Cancer
    ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
    ERD-3111
  • HY-P10446

    Epigenetic Reader Domain PROTACs Cancer
    TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer .
    TAT-PiET-PROTAC
  • HY-137144

    ZB716

    Estrogen Receptor/ERR Cancer
    Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells .
    Fulvestrant-3-boronic acid
  • HY-169903

    Apoptosis Cancer
    SMIP34 is a PELP1 inhibitor. SMIP34 binds to PELP1 with a Kd of 37.4 μM. SMIP34 inhibits cancer cell proliferation and tumor progression. SMIP34 can be used for breast cancer research, and is active against wild-type (WT), mutant (MT) ER+ and therapy-resistant (TR)-ER+ breast cancer .
    SMIP34
  • HY-149295

    PROTACs Estrogen Receptor/ERR Apoptosis Cancer
    PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER + breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
    PROTAC ERα Degrader-4
  • HY-175785

    Estrogen Receptor/ERR Aryl Hydrocarbon Receptor Apoptosis MDM-2/p53 Cancer
    X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer .
    X15695
  • 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 .
    H3B-6545 hydrochloride
  • HY-147402A

    D-0502 meglumine

    Estrogen Receptor/ERR Cancer
    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 .
    Taragarestrant meglumine
  • HY-159613

    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 .
    PELP1-IN-1
  • HY-107835

    FCR 2769

    Environmental Pollutants Apoptosis Bcl-2 Family Parasite Insecticide Infection Cancer
    Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide . Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer .
    Flumethrin
  • HY-145341

    Estrogen Receptor/ERR Cancer
    GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
    GNE-149
  • HY-148368

    Bcl-2 Family Apoptosis Cancer
    CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .
    CYD-4-61
  • HY-177445

    Histone Acetyltransferase Estrogen Receptor/ERR Cancer
    KAT6-IN-4 (Compound Example 2) is a selective lysine acetyltransferase 6 (KAT6) inhibitor. KAT6-IN-4 suppresses transcription of oncogenes like ERα. KAT6-IN-4 demonstrates potent antitumor efficacy in ER +/HER2 - breast cancer xenografts. KAT6-IN-4 is promising for research of KAT6-driven malignancies (e.g., breast cancer, NSCLC) .
    KAT6-IN-4
  • HY-161740

    AUTOTACs Estrogen Receptor/ERR Autophagy Cancer
    PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ .
    PHTPP-1304
  • HY-147402

    D-0502

    Estrogen Receptor/ERR Cancer
    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 .
    Taragarestrant
  • HY-138642S

    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 .
    Vepdegestrant-d5
  • HY-N11785

    Estrogen Receptor/ERR Metabolic Disease Cancer
    Glyceollin I is a selective estrogen receptor (ER) modulator with anticancer, antioxidant, and anti-inflammatory activities. Glyceollin I is promising for research of estrogen-related cancers (e.g., breast, ovarian) and metabolic disorders (e.g., hypercholesterolemia) .
    Glyceollin I
  • HY-W040270

    PROTAC Linkers Cancer
    Amino-PEG10-amine, a PEG-based PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer .
    Amino-PEG10-amine
  • HY-176955

    Estrogen Receptor/ERR Cancer
    ER degrader 12 (Example 1) is an estrogen receptor (ER) degrader with IC50 values for ERα and ERβ of 2.3 and 80.2 nM respectively (TR-FRET experiment). ER degrader 12 inhibits the proliferation of MCF-7 cells, with an IC50 of 1.53 nM. ER degrader 12 can be used for research on breast cancer .
    ER degrader 12
  • HY-174453

    PROTACs Estrogen Receptor/ERR Apoptosis Cancer
    PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)) .
    PROTAC ERα Degrader-12
  • HY-126932

    Estrogen Receptor/ERR Cancer
    TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites .
    TTC-352
  • HY-174870

    PROTACs Estrogen Receptor/ERR Apoptosis Fluorescent Dye Cancer
    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)) .
    PROTAC ERα Degrader-11
  • HY-19822S

    RAD1901-d4

    Isotope-Labeled Compounds Estrogen Receptor/ERR Cancer
    Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
    Elacestrant-d4
  • HY-138642A

    (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 .
    (Rac)-Vepdegestrant
  • HY-179238

    Estrogen Receptor/ERR Cancer
    CS-1-103 is a potent estrogen receptor (ER) inhibitor. CS-1-103 inhibits ER transcriptional activity with an EC50 of 0.36 μM by recruiting methyl-CpG binding domain protein 2 (MBD2), HDACs and the nucleosome remodeling and deacetylase (NuRD) complex. CS-1-103 can be used for breast and prostate cancer research .
    CS-1-103
  • HY-123024

    BL-S-640; SK&F 60771

    Apoptosis Bacterial Antibiotic Infection Cancer
    Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection .
    Cefatrizine
  • HY-130411

    PROTAC Linkers Cancer
    Amino-PEG11-amine, a PEG-based (12 units) PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer .
    Amino-PEG11-amine
  • HY-W288480

    Apoptosis Cancer
    Trihexyl phosphate is an organophosphate flame retardant. Trihexyl phosphate causes mitochondrial impairment and induces cell apoptosis in CHO cells. Trihexyl phosphate promotes the proliferation of human breast cancer cells (MCF-7) in a dose-dependent manner and exerts estrogenicity via ERα-independent pathways .
    Trihexyl phosphate
  • HY-179232

    Estrogen Receptor/ERR Cancer
    ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC50 value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .
    ERα antagonist 2
  • HY-149970

    Estrogen Receptor/ERR Cancer
    ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer .
    ER degrader 5
  • HY-179045

    Estrogen Receptor/ERR Apoptosis Cancer
    ERα degrader 14 (Compound B7) is a potent ERα degrader. ERα degrader 14 exhibits significantly potent and selective anti-proliferative activity on two ERα-positive breast cancer cell lines (MCF-7 and T47D). ERα degrader 14 induces cell cycle arrest, inhibits cell migration, and induces cell apoptosis. ERα degrader 14 effectively inhibits tumor growth in mouse models. ERα degrader 14 can be used for the study of breast cancer .
    ERα degrader 14
  • HY-176486

    Estrogen Receptor/ERR Cancer
    ER degrader 11 (Compound 5) is an orally active, brain-penetrant and selective estrogen receptor (ER) degrader (ERα IC50=1.6 nM). ER degrader 11 is promising for research of breast cancer brain metastasis .
    ER degrader 11
  • HY-172937

    Estrogen Receptor/ERR Cancer
    ERα degrader 13 (compound MR3) is potent ERα degrader with an IC50 of 0.55 μM. ERα degrader 13 induces an obvious tumor regression in the breast cancer xenograft mouse model .
    ERα degrader 13
  • HY-163812

    Molecular Glues Estrogen Receptor/ERR Cancer
    ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .
    ER degrader 9
  • HY-149081

    Estrogen Receptor/ERR Cytochrome P450 Cancer
    ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
    ERα degrader 6

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