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Elacestrant dihydrochloride

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Purity:100%

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COA HNMR HPLC

Elacestrant dihydrochloride

Catalog No. T13675Cas No. 1349723-93-8

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.

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Pack Size	Price	Availability
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

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Product Introduction

Bioactivity

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	ERα:48 nM , ERβ:870 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

Chemical Properties

Molecular Weight	531.56
Formula	C30H40Cl2N2O2
Cas No.	1349723-93-8

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	1.8813 mL	9.4063 mL	18.8126 mL	94.0628 mL
5 mM	0.3763 mL	1.8813 mL	3.7625 mL	18.8126 mL
10 mM	0.1881 mL	0.9406 mL	1.8813 mL	9.4063 mL
20 mM	0.0941 mL	0.4703 mL	0.9406 mL	4.7031 mL
50 mM	0.0376 mL	0.1881 mL	0.3763 mL	1.8813 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0188 mL	0.0941 mL	0.1881 mL	0.9406 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

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