[CAS NO. 1349723-93-8] Elacestrantdihydrochloride

Name: Elacestrantdihydrochloride
Brand: Arctom Scientific
SKU: AS936412

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PRODUCTS SPECIFICATIONS [1349723-93-8]

Distributor

Catalog

AS936412

Brand

Arctom Scientific

CAS

1349723-93-8

DESCRIPTION [1349723-93-8]

Overview

MDL	-
Molecular Weight	531.56
Molecular Formula	C30H40Cl2N2O2
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

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

3 Publications Citing Use of MCE

Summary

Elacestrant dihydrochloride (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC ₅₀ s 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 EC ₅₀ 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 EC ₅₀ of 4 pM. Treatment of cells with RAD1901 in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC ₅₀ 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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00875420	Radius Pharmaceuticals, Inc.	Hot Flashes	March 2009	Phase 2
NCT04797728	SOLTI Breast Cancer Research Group\|Radius Health, Inc.	Breast Cancer\|Hormone Receptor Positive Breast Carcinoma	February 9, 2021	Early Phase 1
NCT05596409	Stemline Therapeutics, Inc.	Metastatic Breast Cancer	January 2023	Phase 2
NCT05386108	Stemline Therapeutics, Inc.	Breast Neoplasms\|Brain Neoplasms\|Neoplasms by Site\|Neoplasms\|Breast Diseases\|Central Nervous System Neoplasms\|Brain Diseases\|Central Nervous System Diseases	August 31, 2022	Phase 1\|Phase 2
NCT02653417	Radius Pharmaceuticals, Inc.	Vasomotor Symptoms\|Hot Flashes	December 2015	Phase 2
NCT05618613	Context Therapeutics Inc.	Breast Cancer	November 22, 2022	Phase 1\|Phase 2
NCT03778931	Stemline Therapeutics, Inc.	Breast Cancer	May 10, 2019	Phase 3
NCT02338349	Stemline Therapeutics, Inc.	Advanced ER&addition;, HER2-Negative Breast Cancer	January 2015	Phase 1
NCT05512364	European Organisation for Research and Treatment of Cancer - EORTC\|Breast International Group\|Menarini Group	ER-positive Breast Cancer\|HER2-negative Breast Cancer\|Stage IIB Breast Cancer\|Stage III Breast Cancer	May 1, 2023	Phase 3
NCT02650817	Stemline Therapeutics, Inc.	Metastatic Breast Cancer	April 1, 2016	Phase 1
NCT05563220	Stemline Therapeutics, Inc.	Breast Cancer\|Metastatic Breast Cancer	December 31, 2022	Phase 1\|Phase 2
NCT04791384	Criterium, Inc.	Breast Cancer	April 21, 2022	Phase 1\|Phase 2

Appearance

Solid

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)

H ₂ O : 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.

References

[1] Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56.