Tamoxifen-d₃ hydrochloride  (Synonyms: ICI 46474-d₃ hydrochloride; (Z)-Tamoxifen-d₃ hydrochloride; trans-Tamoxifen-d₃ hydrochloride)

Tamoxifen-d₃ hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells^[1][2][3].Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC₅₀ of 0.1 μM and 1.8 μM, respectively^[5]. Tamoxifen Citrate activates autophagy and induces apoptosis^[4].Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse^[6].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
Tamoxifen Citrate (ICI 46474) shows strong inhibition of MCF-7 cells (EC₅₀=1.41 μM) and to a lesser extent the T47D cells (EC₅₀=2.5 μM) but does not affect the MDA-MB-231 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

410.99

C₂₆H₂₇D₃ClNO

54965-24-1

Solid

White to off-white

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C([2H])([2H])[2H])C)C=C2)\C3=CC=CC=C3.Cl

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.  [Content Brief]

  [3]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.  [Content Brief]

  [4]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.  [Content Brief]

  [5]. Feil S, et, al. Inducible Cre mice. Methods Mol Biol. 2009;530:343-63.  [Content Brief]

  [6]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.  [Content Brief]

  [7]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.  [Content Brief]