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Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant is an orally available selective estrogen receptor degrader .

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $126 | In Stock | In Stock | |
| 5 mg | $247 | In Stock | In Stock | |
| 10 mg | $396 | In Stock | In Stock | |
| 25 mg | $679 | In Stock | In Stock | |
| 50 mg | $960 | In Stock | In Stock | |
| 100 mg | $1,280 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $248 | In Stock | In Stock |
| Description | Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant is an orally available selective estrogen receptor degrader . |
| Targets&IC50 | ERα:48 nM , ERβ:870 nM |
| 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. |
| Synonyms | RAD1901 |
| Molecular Weight | 458.63 |
| Formula | C30H38N2O2 |
| Cas No. | 722533-56-4 |
| Smiles | CCNCCc1ccc(CN(CC)c2cc(OC)ccc2[C@@H]2CCc3cc(O)ccc3C2)cc1 |
| Relative Density. | 1.111 g/cm3 (Predicted) |
| 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. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.72 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 | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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