Elacestrant (RAD1901) Dihydrochloride

Catalog No.S9629 Batch:S962901

Print

Technical Data

Formula

C30H40Cl2N2O2
Molecular Weight 531.56 CAS No. 1349723-93-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (188.12 mM)
Water 25 mg/mL (47.03 mM)
Ethanol 6 mg/mL (11.28 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Elacestrant (RAD1901) Dihydrochloride is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively.
Targets
ERα [1] ERβ [1]
48 nM 870 nM
In vitro

Elacestrant (RAD1901) Dihydrochloride is a selective estrogen receptor degradation (SERD), which inhibits expression of ERα and ERβ in cultured breast tumor cell lines, thus inhibits the cell proliferation in a dose-dependent manner.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MCF-7 cells

  • Concentrations

    0.5-10 μM

  • Incubation Time

    48 h

  • Method

    ERα expression in MCF-7 cells in the presence of vehicle (0.1% DMSO), E2 (1 nmol/l), fulvestrant (100 nmol/l), tamoxifen (1 μmol/l), or RAD1901 (10 μmol/l to 0.5 nmol/l)  for 48 h. Levels of ERα receptor expression are expressed as percent of vehicle control.

Selleck's Elacestrant (RAD1901) Dihydrochloride has been cited by 1 publication

Activity of Estrogen Receptor β Agonists in Therapy-Resistant Estrogen Receptor-Positive Breast Cancer [ Front Oncol, 2022, 12:857590] PubMed: 35574319

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.