2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Elacestrant dihydrochloride

Elacestrant dihydrochloride  (Synonyms: RAD1901 dihydrochloride)

Cat. No.: HY-19822A Purity: 99.72%
COA Handling Instructions

Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.

For research use only. We do not sell to patients.

Elacestrant dihydrochloride Chemical Structure

Elacestrant dihydrochloride Chemical Structure

CAS No. : 1349723-93-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 357 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 357 In-stock
Solid
1 mg USD 150 In-stock
5 mg USD 305 In-stock
10 mg USD 490 In-stock
50 mg USD 1570 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Elacestrant dihydrochloride:

Elacestrant dihydrochloride Related Antibodies

Top Publications Citing Use of Products

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo[1][2].

IC50 & Target

IC50: 48 nM (ERα), 870 nM (ERβ)[1]
In Vitro

Elacestrant dihydrochloride (RAD1901; 0.5 nM-10 µM; 48 h) exhibits dose-dependent inhibition of ERα expression, with a EC50 of 0.6 nM in MCF-7 cells[1].
Elacestrant dihydrochloride (0-1 µM; 48 h) inhibits proliferation of Estradiol (E2)-stimulated MCF-7 cells in a dose-dependent manner, with an EC50 of 4 pM[1].
Elacestrant dihydrochloride (0-1 µM; 24 or 48 h) results in a dose-dependent and marked decrease in estrogen receptor protein expression in MCF7, T47D, and HCC1428 cells[2].
Elacestrant dihydrochloride (0.01, 0.1, 1.0 µM) decreases expression of progesterone receptor (PGR, PR; an ER target gene), in both MCF7 and T47D cell lines[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Elacestrant dihydrochloride Related Antibodies

Cell Proliferation Assay[1]

Cell Line: ER-positive MCF-7 cells (Estradiol (E2)-stimulated)
Concentration: 0-1 µM
Incubation Time: 48 h
Result: Showed antiproliferative activity on cells.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.5 nM-10 µM
Incubation Time: 48 h
Result: Inhibited ERα expression (EC50 of 0.6 nM) in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: MCF7, T47D, and HCC1428 cells
Concentration: 0-1 µM
Incubation Time: 24 or 48 h
Result: Decreased the expression of estrogen receptor protein.
In Vivo

Elacestrant dihydrochloride (0.3-120 mg/kg; p.o.; single daily for 40 days) antagonizes E2-mediated uterine stimulation in a dose-dependent manner in vivo[1].
Elacestrant dihydrochloride (30, 60 mg/kg; p.o.; single daily for 4 weeks) induces complete tumor growth inhibition in mice[2].
Tumor growth inhibition is maintained for 4 weeks after Elacestrant dihydrochloride withdrawal[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MCF7 cell line xenograft model of mice[2].
Dosage: 30, 60 mg/kg
Administration: Oral administration; single daily for 4 weeks.
Result: Inhibited growth of tumor.
Clinical Trial
Molecular Weight

531.56

Appearance

Solid

Formula

C30H40Cl2N2O2
CAS No.
SMILES

OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC)CC4=CC=C(CCNCC)C=C4)CCC2=C1.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (188.13 mM; Need ultrasonic)

H2O : 50 mg/mL (94.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8813 mL 9.4063 mL 18.8126 mL
5 mM 0.3763 mL 1.8813 mL 3.7625 mL
10 mM 0.1881 mL 0.9406 mL 1.8813 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.87 mg/mL (5.40 mM); Clear solution

  • 2.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.87 mg/mL (5.40 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

  • 5.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

  • 6.

    Add each solvent one by one:  1% DMSO    99% saline

    Solubility: ≥ 0.57 mg/mL (1.07 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.72%

COA (249 KB) LCMS (261 KB)

Handling Instructions (2659 KB)
References
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Elacestrant dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Elacestrant1349723-93-8RAD1901RAD 1901RAD-1901Estrogen Receptor/ERRbreast cancerERestrogen receptorMCF7 cellsT47D cellsHCC1428 cellsInhibitorinhibitorinhibit

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