Elacestrant-d4

Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822) . Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER+ breast cancer cell lines both in vitro and in vivo.

Product Specifications

Product Name Alternative

RAD1901-d4

UNSPSC

12352005

Target

Estrogen Receptor/ERR; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

Others; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Solubility

10 mM in DMSO

Smiles

OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC)CC4=CC=C(CC([2H])([2H])NC([2H])([2H])C)C=C4)CCC2=C1

Molecular Formula

C30H34D4N2O2

Molecular Weight

462.66

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Bihani T, et al. Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), Has Antitumor Activity in Multiple ER+ Breast Cancer Patient-derived Xenograft Models. Clin Cancer Res. 2017 Aug 15;23 (16) :4793-4804.|[3]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.