| Name | Elacestrant |
| Description | Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant is an orally available selective estrogen receptor degrader . |
| In vitro | Elacestrant treatment exhibits dose-dependent inhibition of ERα expression, with an EC50 of 0.6 nM.Treatment of ER-positive MCF-7 cells with E2 results in a potent and dose-dependent increase in proliferation, with an EC50 of 4 pM.Treatment of cells with Elacestrant in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM.Elacestrant selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. |
| In vivo | Elacestrant produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models.Elacestrant preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2.Elacestrant-treated animals survived longer than those treated with either control or fulvestrant. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 150 mg/mL (327.06 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (8.72 mM), Sonication is recommended.
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| Keywords | RAD-1901 | RAD 1901 | progestogenReceptor | progestogen Receptor | Inhibitor | inhibit | EstrogenReceptor | Estrogen Receptor/ERR | Estrogen Receptor | ERβ | ERα | ERR | Elacestrant |
| Inhibitors Related | Tamoxifen | Mifepristone | Estradiol | Astragaloside IV | Progesterone | Bisphenol B | Mequinol | Phthalic acid | Ethisterone | Alpha-Estradiol | Ferrous Bisglycinate | Cholesterol |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Ovarian Cancer Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
