Elacestrant , also known as RAD1901, 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 RAD1901, 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, RAD1901 is able to cross the blood-brain barrier (BBB).
| Catalog Number | I006453 |
| CAS Number | 1349723-93-8 (HCl) |
| Synonyms | RAD1901; RAD-1901; RAD 1901; RAD1901 HCl salt; Elacestrant dihydrochloride;(R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride |
| Molecular Formula | C30H40Cl2N2O2 |
| Purity | 95% |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4°C for short term or -20 °C for long term |
| 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 |
| InChIKey | XGFHYCAZOCBCRQ-FBHGDYMESA-N |
| SMILES | OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC4=CC=C(CCNCC)C=C4)CC)CCC2=C1.[H]Cl.[H]Cl |
| Reference | </br>1:Garner F, Shomali M, Paquin D, Lyttle CR, Hattersley G. 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. doi: 10.1097/CAD.0000000000000271. PubMed PMID: 26164151; PubMed Central PMCID: PMC4560273.</br>2:Wardell SE, Nelson ER, Chao CA, Alley HM, McDonnell DP. Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader. Endocr Relat Cancer. 2015 Oct;22(5):713-24. doi: 10.1530/ERC-15-0287. Epub 2015 Jul 10. PubMed PMID: 26162914; PubMed Central PMCID: PMC4545300. |
