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Elacestrant dihydrochloride (Synonyms: RAD1901 dihydrochloride)

Cat. No.: HY-19822A Purity: 99.81%
Handling Instructions

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

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
10 mM * 1 mL in DMSO USD 491 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Elacestrant dihydrochloride:

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Description

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

IC50 & Target

IC50: 48 nM (ERα), 870 nM (ERβ)[1]

In Vitro

RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. RAD1901 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 RAD1901 in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM[1].

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

In Vivo

RAD1901 produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models. RAD1901-treated animals survived longer than those treated with either control or ICI 182780. RAD1901 preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2[1].

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

Clinical Trial
Molecular Weight

531.56

Formula

C₃₀H₄₀Cl₂N₂O₂

CAS No.

1349723-93-8

SMILES

OC1=CC=C2C[[email protected]](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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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:  1% DMSO    99% saline

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

  • 2.

    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

  • 3.

    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

  • 4.

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

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

  • 5.

    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

  • 6.

    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

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

For proliferation assays, MCF-7 cells are treated with 2% charcoal-stripped FBS–MEM containing 10 pM E2 with either RAD1901 or additional E2 at concentrations ranging from 10-9 to 1 M. The medium is removed after 48 h of incubation and the cells are lysed by adding 100 μl of CellTiter Glo. The plates are gently mixed on a plate shaker for 10 min before the luminescent signal is measured on a luminometer. The EC50 and IC50of the test compound are then defined[1].

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

Animal Administration
[1]

Mice: RAD1901 is stored as a dry powder, formulated for use as a homogenous suspension in 0.5% (w/v) methylcellulose in deionized water. Fourteen days after tumor cell implantation, the mice are randomized into nine groups of 15 animals each and treated with vehicle, CI 47699 (1 mg/animal every other day), ICI 182780 (0.5 mg/animal daily), or RAD1901 (0.3, 1, 3, 10, 30, 60, 90, and 120 mg/kg daily). Tumor volumes are evaluated twice per week[1].

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

References

Purity: 99.81%

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Keywords:

ElacestrantRAD1901RAD 1901RAD-1901Estrogen Receptor/ERRInhibitorinhibitorinhibit

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Product Name:
Elacestrant dihydrochloride
Cat. No.:
HY-19822A
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