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Elacestrant dihydrochloride
- RAD1901
- Parent CAS: 722533-56-4
- Optical Purity: 100% e.e.
- Soluble in water and DMSO
- MF: C30H38N2O2.2HCl
- MW: 531.56
Description
Elacestrant dihydrochloride is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 values of 48 nM and 870 nM for ERα and ERβ, respectively. Elacestrant is a potent antagonist of breast cancer cells, inhibiting both basal and E2-stimulated MCF-7 cell proliferation.
More Information
| Parent CAS No. | 722533-56-4 |
|---|---|
| Chemical Name | (R)-6-(2-(Ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride |
| SMILES | C1C=C2C[C@H](C3C(N(CC)CC4C=CC(CCNCC)=CC=4)=CC(OC)=CC=3)CCC2=CC=1O.Cl.Cl |&1:4,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C30H38N2O2/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/t26-/m1/s1 |
| InChiKey | SIFNOOUKXBRGGB-AREMUKBSSA-N |
| CID | 23642301 |
| Short Description | SERD |
References
- SE Wardell et al. Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader. Endocr Relat Cancer. 2015 Oct;22(5):713-24.
- F Garner 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.
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