Elacestrant [722533-56-4]

Référence T13674-1mg

Conditionnement : 1mg

Marque : TargetMol

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Elacestrant

(Synonyms: RAD1901) Copy Product Info
Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader .
Elacestrant
Cas No. 722533-56-4
Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.92%
Appearance:Solid
Color:White
COA LCMS HNMR

Product Introduction

Bioactivity
Description
Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader .
Targets & IC50
ERα:48 nM , ERβ:870 nM
In vitro
Elacestrant 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 Elacestrant in the presence of 10 pM E2 resultsin 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.
In vivo
Elacestrant produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models.Elacestrant preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2.Elacestrant-treated animals survived longer than those treated with either control or fulvestrant.
SynonymsRAD1901
Chemical Properties
Molecular Weight458.63
FormulaC30H38N2O2
Cas No.722533-56-4
SmilesCCNCCc1ccc(CN(CC)c2cc(OC)ccc2[C@@H]2CCc3cc(O)ccc3C2)cc1
Relative Density.1.111 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 150 mg/mL (327.06 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.72 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1804 mL10.9020 mL21.8041 mL109.0203 mL
5 mM0.4361 mL2.1804 mL4.3608 mL21.8041 mL
10 mM0.2180 mL1.0902 mL2.1804 mL10.9020 mL
20 mM0.1090 mL0.5451 mL1.0902 mL5.4510 mL
50 mM0.0436 mL0.2180 mL0.4361 mL2.1804 mL
100 mM0.0218 mL0.1090 mL0.2180 mL1.0902 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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