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Elacestrant dihydrochloride

Catalog No. T13675 CAS 1349723-93-8

Synonyms: RAD1901 dihydrochloride

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Elacestrant dihydrochloride Chemical Structure

Elacestrant dihydrochloride, CAS 1349723-93-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 122.00
5 mg	In stock	$ 249.00
10 mg	In stock	$ 396.00
25 mg	In stock	$ 665.00
50 mg	In stock	$ 947.00
100 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 293.00

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Purity: 100%

Purity: 98.46%

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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	ERβ:870 nM , ERα:48 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].?

Synonyms	RAD1901 dihydrochloride
Molecular Weight	531.56
Formula	C30H40Cl2N2O2
CAS No.	1349723-93-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (150.50 mM), Sonication is recommended.

H2O: 40 mg/mL (75.25 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Clinical Compound Library Approved Drug Library Anti-Breast Cancer Compound Library FDA-Approved & Pharmacopeia Drug Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Keywords

Elacestrant dihydrochloride 1349723-93-8 Endocrinology/Hormones Estrogen/progestogen Receptor inhibit RAD-1901 Dihydrochloride Inhibitor Elacestrant Dihydrochloride RAD1901 Dihydrochloride Estrogen Receptor/ERR Elacestrant RAD 1901 Dihydrochloride RAD1901 RAD 1901 RAD-1901 RAD1901 dihydrochloride inhibitor

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