Elacestrant

• CAT Number: I013691
• CAS Number: 722533-56-4
• Molecular Formula: C₃₀H₃₈N₂O₂
• Molecular Weight: 458.63
• Purity: 98%
• Target: Estrogen Receptor/ERR
• Target Protein: P03372
• Solubility: DMSO
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: IC50: 48 nM (ERα), 870 nM (ERβ)
• IUPAC Name: (6R)-6-[2-[ethyl-[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydronaphthalen-2-ol
• 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
• SMILES: CCNCCC1=CC=C(C=C1)CN(CC)C2=C(C=CC(=C2)OC)[C@@H]3CCC4=C(C3)C=CC(=C4)O

Elacestrant（Cat No.:I013691）is an oral selective estrogen receptor degrader (SERD) developed for the treatment of estrogen receptor-positive (ER+), HER2-negative advanced or metastatic breast cancer. It works by binding to the estrogen receptor (ER) and promoting its degradation, effectively reducing estrogen signaling, which drives cancer cell growth in ER+ breast cancer. Elacestrant offers a targeted approach for patients who have progressed on other endocrine therapies, such as aromatase inhibitors or selective estrogen receptor modulators (SERMs). Its oral administration provides a convenient alternative to injectable SERDs.

Reference

[1]. Garner F, 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.