Home Endocrinology & Hormones Estrogen/progestogen Receptor modulator Toremifene Citrate (NK 622) For research use only.

Toremifene Citrate (NK 622)

Synonyms: NSC 613680,NK 622 Citrate

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

Toremifene Citrate (NK 622) Chemical Structure

Toremifene Citrate (NK 622) Chemical Structure

CAS No. 89778-27-8

Purity & Quality Control

Toremifene Citrate (NK 622) Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

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.
Targets
Estrogen receptor [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01214291 Withdrawn
Risk of Bone Fracture Occurrences
GTx|Ipsen
 March 2011 Phase 3
NCT00267553 Terminated
Breast Neoplasms|Neoplasms Hormone-Dependent
Intarcia Therapeutics
 November 2005 Phase 3
NCT00106691 Completed
Preneoplastic Conditions|Prostatic Intraepithelial Neoplasia
GTx
 January 2005 Phase 3

Chemical Information & Solubility

Molecular Weight 598.08 Formula

C32H36ClNO8
CAS No. 89778-27-8 SDF Download Toremifene Citrate (NK 622) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 120 mg/mL ( (200.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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