A selective estrogen receptor degrader
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Elacestrant (hydrochloride)

Item No. 37298

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6R-[2-[ethyl[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydro-2-naphthalenol, dihydrochloride
CAS Number
1349723-93-8
Synonyms
  • RAD901
Molecular Formula
C30H38N2O2 • 2HCl
Formula Weight
531.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CCNCCC1=CC=C(CN(C2=CC(OC)=CC=C2[C@H]3CC4=CC=C(O)C=C4CC3)CC)C=C1.Cl.Cl
InChi Code
InChI=1S/C30H38N2O2.2ClH/c1-4-31-17-16-22-6-8-23(9-7-22)21-32(5-2)30-20-28(34-3)14-15-29(30)26-11-10-25-19-27(33)13-12-24(25)18-26;;/h6-9,12-15,19-20,26,31,33H,4-5,10-11,16-18,21H2,1-3H3;2*1H/t26-;;/m1../s1
InChi Key
XGFHYCAZOCBCRQ-FBHGDYMESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $40

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    1 mg

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    5 mg

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    10 mg

    $590

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    Cayman Chemical
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    Product Description

    Elacestrant is a selective estrogen receptor degrader (SERD).1 It selectively binds to estrogen receptor α (ERα) over ERβ (IC50s = 48 and 870 nM, respectively) and reduces ERα levels in MCF-7 cells (EC50 = 0.6 nM). Elacestrant reduces MCF-7 proliferation induced by 17β-estradiol (E2; Item No. 10006315) (EC50 = 4 pM). In vivo, elacestrant (30 and 60 mg/kg) reduces E2-induced tumor growth in an MCF-7 mouse xenograft model. It increases survival in an MCF-7 intracranial mouse xenograft model. Elacestrant (0.1-3 mg/kg) protects against bone loss in ovariectomized rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Garner, F., Shomali, M., Paquin, D., et al. RAD1901: A novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs 26(9), 948-956 (2015).