Elacestrant dihydrochloride

Elacestrant dihydrochloride (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.

Product information

CAS Number: 1349723-93-8

Molecular Weight: 531.56

Formula: C30H40Cl2N2O2

Chemical Name: (6R)-6-{2-[ethyl({4-[2-(ethylamino)ethyl]phenyl}methyl)amino]-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride

Smiles: Cl.Cl.COC1=CC(=C(C=C1)[C@H]1CC2=CC=C(O)C=C2CC1)N(CC1C=CC(CCNCC)=CC=1)CC

InChiKey: XGFHYCAZOCBCRQ-FBHGDYMESA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (188.13 mM; Need ultrasonic). H2O : 50 mg/mL (94.06 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. RAD1901 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 RAD1901 in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM.

In Vivo:

RAD1901 produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models. RAD1901-treated animals survived longer than those treated with either control or ICI 182780. RAD1901 preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2.

Products are for research use only. Not for human use.