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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $122 | In Stock | In Stock | |
| 5 mg | $249 | In Stock | In Stock | |
| 10 mg | $396 | In Stock | In Stock | |
| 25 mg | $665 | In Stock | In Stock | |
| 50 mg | $947 | In Stock | In Stock | |
| 100 mg | $1,280 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $293 | In Stock | In Stock |
| 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. |
| Targets&IC50 | ERα:48 nM , ERβ:870 nM |
| 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].? |
| Synonyms | RAD1901 dihydrochloride |
| Molecular Weight | 531.56 |
| Formula | C30H40Cl2N2O2 |
| Cas No. | 1349723-93-8 |
| Smiles | Cl.Cl.CCNCCc1ccc(CN(CC)c2cc(OC)ccc2[C@@H]2CCc3cc(O)ccc3C2)cc1 |
| Relative Density. | no data available |
| 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. H2O: 40 mg/mL (75.25 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.76 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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