Toremifene Citrate

Toremifene Citrate

Toremifene CitrateOncology
CAS: 89778-27-8
MF: C26H28ClNO.C6H8O7
MW: 598.08
Indications
Breast Neoplasms;Ovarian Neoplasms;Precancerous Conditions;Prostatic Intraepithelial Neoplasia;Fractures, Bone;Osteoporosis;Prostatic Neoplasms
Therapeutic Target
ERs
Usage

A selective estrogen receptor modulator (SERM). It is used to treat metastatic breast cancer in postmenopausal women with estrogen receptor - positive or unknown status, and exerts its effects by regulating estrogen receptors.

Specification
>99%
Product Description

Overview

Toremifene Citrate is a potent oral non - steroidal selective estrogen receptor modulator (SERM), which exerts the effect of regulating estrogen receptors (mainly exhibiting anti - estrogen activity in specific tissues). Toremifene Citrate can be used for the treatment of metastatic breast cancer in postmenopausal women with estrogen receptor - positive or unknown status, and also for research on estrogen - related disorders.

Synonyms: GTx-006; FC 1157; FC-1157a; NK-622; Estrimex; Acapodene; (z)-4-chloro-1,2-diphenyl-1-(4-(2-(n,n-dimethylamino)ethoxy)phenyl)-1-butene; 2-(4-(4-chloro-1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethyl-ethanamin(z)-ethanamin; 2-hydroxy-1,2,3-propanetricarboxylate(1:1); fareston; fc1157a; nk622; TOREMIFENE CITRATE; (z)-2-[4-(4-chloro-1,2-diphenyl-1-butenyl)phenoxy]-n,n-dimethyl-ethanamine 2-hydroxy-1,2,3-propanetricarboxylate

EINECS: 663-344-6

Product Categories: XYREM; Analgesics; Active Pharmaceutical Ingredients; Amines; Aromatics; Inhibitors; Intermediates & Fine Chemicals; Pharmaceuticals

Mol File: 89778-27-8.mol

Physicochemical Properties

Melting point: 160-162°C

Boiling point : 146-148C

Storage temp: 2-8°C

Solubility: DMSO: >10mg/mL

Form: powder

Color: White to Off-white

Stability: Light Sensitive

MSDS Information

Experimental Data

1.Cell Experiment

Solubility in DMSO : ≥ 100 mg/mL (167.20 mM; Hygroscopic DMSO has a significant effect on the solubility of the product, use freshly opened DMSO);H2Solubility in O : < 0.1 mg/mL (insoluble);"≥" means soluble, but saturation unknown.

Preparing Stock Solutions:

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Please choose the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; Once prepared into a solution, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and duration of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。 Use within 6 months when stored at -80°C, and within 1 month when stored at -20°C.


2. Animal Experiment

Choose the appropriate dissolution protocol based on your experimental animal and mode of administration.For the following dissolution schemes, please prepare the clarified stock solution according to the in vitro method, and then add the co-solvent in turn:


- In order to ensure the reliability of the experimental results, the clarified stock solution can be properly stored according to the storage conditions; It is recommended that you use the working solution for in vivo experiments and use it on the same day;The percentages shown before the following solvents are the proportion of the volume of that solvent in your final solution; If precipitation and precipitation occur during the preparation process, it can be dissolved by heating and/or ultrasound.


Option 1

Add each solvent in order: 10% DMSO ,   40% PEG300 , 5% Tween-80, 45% Saline.

Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear Solution

A clarified solution of ≥ 2.5 mg/mL (saturation unknown) is obtained for this protocol.

For example, take 1 mL of working solution and add 100 μL of 25.0 mg/mL of clarified DMSO stock solution to 400 μL of PEG300 and mix well. Add 50 μL of Tween-80 to the above system and mix well; Then proceed with 450 μL of normal saline to 1 mL.

Preparation of normal saline: 0.9 g of sodium chloride dissolved in ddH₂O and fixed to 100 mL can obtain a clear and transparent normal saline solution.


Option 2

add each solvent in order: 10% DMSO; 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear Solution.

A clarified solution of ≥ 2.5 mg/mL (saturation unknown) is obtained for this protocol.

For example, take 1 mL of working solution and add 100 μL of 25.0 mg/mL of clarified DMSO stock solution to 900 μL of 20% SBE-β-CD saline aqueous and mix well.2 g of SBE-β-CD (sulfonbutyl ether β-cyclodextrin) powder is set in 10 mL of normal saline and completely dissolved until clear.


Option 3

Add each solvent in order:10% DMSO , 90% Corn Oil

Solubility:  ≥ 2.5 mg/mL (4.18 mM); Clear solution

A clarified solution of ≥ 2.5 mg/mL (saturation unknown) is available for this protocol, as appropriate for animal experiments with experimental cycles of more than half a month.

For example, 100 μL of 25.0 mg/mL of clarified DMSO stock solution is added to 900 μL of corn oil and mixed well.

Pharmacodynamics


Mechanism Of Action