Elacestrant-d6

• UNSPSC Description:

  Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant 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.

• Target Antigen:

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

• Molecular Weight:

  464.67

• 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.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported