| Name | Elacestrant dihydrochloride |
| Description | 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. |
| In vitro | Elacestrant exhibits inhibition of ERα expression in a dose-dependent manner, 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 results in 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[1].? |
| In vivo | In MCF-7 xenograft models, Elacestrant-treated animals survived longer than those treated with either control or ICI 182780. RAD1901 preserves ovariectomy-induced bone loss and prevents the uterotropic effects of E2. Elacestrant produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models[1].? |
| 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 : 55 mg/mL (103.47 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.76 mM), Sonication is recommended.
H2O : 40 mg/mL (75.25 mM), Sonication is recommended.
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| Keywords | RAD-1901 Dihydrochloride | RAD1901 Dihydrochloride | RAD-1901 | RAD1901 | RAD 1901 Dihydrochloride | RAD 1901 | progestogenReceptor | progestogen Receptor | Inhibitor | inhibit | EstrogenReceptor | Estrogen Receptor/ERR | Estrogen Receptor | ERβ | ERα | Elacestrant Dihydrochloride | Elacestrant |
| Inhibitors Related | Tamoxifen | Mifepristone | Estradiol | Astragaloside IV | Bisphenol B | Bisphenol Z | Mequinol | Phthalic acid | Ethisterone | Alpha-Estradiol | Ferrous Bisglycinate | Cholesterol |
| Related Compound Libraries | Bioactive Compound Library | Approved Drug Library | Anti-Breast Cancer Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Endocrinology-Hormone Compound Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
