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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 | Availability | Quantity |
---|---|---|---|
1 mg | $122 | In Stock | |
5 mg | $249 | In Stock | |
10 mg | $396 | In Stock | |
25 mg | $665 | In Stock | |
50 mg | $947 | In Stock | |
100 mg | $1,280 | In Stock | |
1 mL x 10 mM (in DMSO) | $293 | 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 | ERβ:870 nM , ERα:48 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].? |
Alias | 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. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (103.47 mM), Sonication is recommended. H2O: 40 mg/mL (75.25 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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