| S1304 |
Megestrol Acetate
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Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
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Scientific Reports, October 06, 2017, 12754
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OncoTargets and Therapy, October 03, 2017, 4809-4819
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iScience, 2024, 27(10):110862
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| S8372 |
AZD9496
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AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
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Breast Cancer Research, August 14, 2023, 96
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Breast Cancer Research and Treatment, April 2020, 635-646
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ACS Omega, 2025, 10(15):15256-15271
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| S5910 |
Alpha-Estradiol
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Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen.
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Biomater Res, 2024, 28:0010
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| E5720 |
Isocurcumenol
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Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1μg/mL and 178.2 μg/mL in DLA and KB cells, respectively.
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| E4621 |
BHPI
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BHPI is a potent noncompetitive inhibitor of estrogen receptor α (ERα), which disrupts the protective estrogen–ERα-mediated activation of the unfolded protein response (UPR), leading to sustained UPR activation. It specifically inhibits the growth of drug-resistant ERα-positive breast and ovarian cancer cells and induces significant tumor regression in a mouse xenograft model of breast cancer.
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| S5454 |
Saikosaponin D
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Saikosaponin D, a calcium mobilizing agent (SERCA inhibitor), is a type of Saponin derivative, which is a component extracted from Bupleurum falactum. This compound has anti-cancer activities.
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Scientific Reports, 2026, Vol 16, Article number: 1
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Theranostics, 2025, 8935-8951
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Theranostics, 2025, 15(17):8935-8951
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| E7992 |
Endoxifen
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Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.
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| E2401 |
SPP-86
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SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
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| S3284 |
Tracheloside
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Tracheloside is a lignan glycoside isolated from seeds of Carthamus tinctorius with anti-estrogenic effects. This compound significantly decreases the activity of alkaline phosphatase (AP) (an estrogen-inducible marker enzyme) with IC50 of 0.31 μg/ml. It promotes keratinocyte proliferation through ERK1/2 stimulation.
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