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Elacestrant

Elacestrant structure

CAS No:
722533-56-4
Formula:
C30H38N2O2
Chemical Name:
Elacestrant
Synonyms:
Elacestrant;Elacestrant (RAD1901);Elacestrant ISO 9001：2015 REACH;inhibit,RAD 1901,Estrogen Receptor/ERR,Inhibitor,Elacestrant,RAD-1901;Venadaparib Impurity 54;(6R)-6-2-ethyl(4-2-(ethylamino)ethylphenylmethyl)amino-4-methoxyphenyl-5,6,7,8-tetrahydronaphthalen-2-ol;(R)-6-[2-[Ethyl[4-[2-(ethylamino)ethyl]benzyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydronaphthalen-2-ol;Elacestrant - API standards
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Elacestrant is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. Upon oral administration of higher doses of elacestrant, this agent acts as a SERD, which binds to the estrogen receptor (ER) and induces a conformational change that results in the degradation of the receptor. This may inhibit the growth and survival of ER-expressing cancer cells. At lower doses of this agent, RAD1901 acts as a SERM and has estrogen-like effects in certain tissues, which can both reduce hot flashes and protect against bone loss. In addition, elacestrant is able to cross the blood-brain barrier (BBB).

Elacestrant Basic Attributes

Molecular Weight：

458.63

Exact Mass：

458.293328459

EC Number：

258-984-3

UNII：

FM6A2627A8

NCI Thesaurus Code：

C120211

Color/Form：

White to off-white

Characteristics

Density：

1.111±0.06 g/cm3(Predicted)

Boiling Point：

609.5±55.0 °C(Predicted)

PKA：

10.36±0.40(Predicted)

Drug Information

Drug Indication：

Investigated for use/treatment in menopause and female hormonal deficiencies/abnormalities.

Mechanism of Action：

RAD1901 is a novel selective estrogen receptor modulator(SERM). SERMs are small molecules that bind to and selectively modulate estrogen receptors. These molecules have the ability to stimulate or block estrogen's activity in different types of tissue, functioning as estrogen receptor agonists in some tissues and as estrogen receptor antagonists in others. RAD1901 has potential to reduce vasomotor symptoms, along with a simultaneous bone-protective effect, without stimulating breast or uterine tissues. RAD1901 is distinctive from other SERMs in its unique biological profile, combined with its significant ability to penetrate the blood-brain barrier, which enables RAD1901 to function as an estrogen agonist within the central nervous system and thereby relieve hot flashes.

MeSH Entry Terms：

(6R)-6-(2-(ethyl((4-(2-(ethylamino)ethyl)phenyl)methyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol

Elacestrant Use and Manufacturing

Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo[1][2].

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CAS No.: 722533-56-4

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