Toremifene Citrate (NK 622)

For research use only.

Catalog No.S1776 Synonyms: NSC 613680

8 publications

Toremifene Citrate (NK 622) Chemical Structure

CAS No. 89778-27-8

Toremifene Citrate (NK 622, NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.

Selleck's Toremifene Citrate (NK 622) has been cited by 8 publications

2 Customer Reviews

  • Representative images of OPCs treated for 72 h with the indicated small molecules. All molecules were used at 300 nM. Scale bar, 100 μm.

    Nature, 2018, 560(7718):372-376. Toremifene Citrate (NK 622) purchased from Selleck.

    D: Marginal degradation of MGMT in MCF7 cells treated with toremifene, a SERM. MGMT: O6-methylguanine DNA-methyltransferase; C: control.

    J Biomed Res, 2016, 30(5): 393-410.. Toremifene Citrate (NK 622) purchased from Selleck.

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Toremifene Citrate (NK 622, NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.
Estrogen receptor [1]
In vitro

Toremifene (7.5 mM) causes approximately 60% of the cells to exhibit morphologic characteristics typical of cells undergoing programmed death, or apoptosis in human breast cancer cells. Toremifene (5-10 mM) results in elevated levels of TRPM-2 and TGF beta 1 mRNAs in in vitro or in vivo grown tumor cells. Toremifene causes growth inhibition of estrogen-sensitive breast cancer cells by inducing some cells to undergo apoptosis and by inhibiting other cells from entering mitosis. [1] Toremifene induces a dose-dependent level of adducts that is lower than that observed for TAM. Toremifene significantly enhances endogenous DNA adduct formation. [2] Toremifene affects the cell turnover by inhibiting mitotic activity and modifying abundant spontaneous apoptosis in DMBA-induced rat mammary carcinoma. [3]

In vivo Toremifene, at the highest tested dose, increases the incidence of hepatocellular carcinomas in the DEN-initiated groups to a level one-third that observed with Tamoxifen administration to DEN-initiated rats. Toremifene increases the incidence of hypernephromas in previously DEN-initiated rats. [4] Toremifene results in aneuploidy in 50% of the cells examined and compared with the 85% level induced by Tamoxifen in female Sprague-Dawley rats. [5]


Solubility (25°C)

In vitro DMSO 100 mg/mL (167.2 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 598.08


CAS No. 89778-27-8
Storage powder
in solvent
Synonyms NSC 613680
Smiles CN(C)CCOC1=CC=C(C=C1)C(=C(CCCl)C2=CC=CC=C2)C3=CC=CC=C3.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01214291 Withdrawn Drug: Toremifene Risk of Bone Fracture Occurrences GTx|Ipsen March 2011 Phase 3
NCT00267553 Terminated Drug: Atamestane|Drug: toremifene|Drug: letrozole Breast Neoplasms|Neoplasms Hormone-Dependent Intarcia Therapeutics November 2005 Phase 3
NCT00106691 Completed Drug: Toremifene 20 mg|Drug: Placebo Preneoplastic Conditions|Prostatic Intraepithelial Neoplasia GTx January 2005 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID