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[CAS NO. 54965-24-1]  TamoxifenCitrate

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PRODUCTS SPECIFICATIONS [54965-24-1]

Catalog
AS987133
Brand
Arctom Scientific
CAS
54965-24-1

DESCRIPTION [54965-24-1]

Overview

MDL-
Molecular Weight563.64
Molecular FormulaC32H37NO8
SMILESCC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)\C3=CC=CC=C3.O=C(CC(C(O)=O)(O)CC(O)=O)O

For research use only. We do not sell to patients.

46 Publications Citing Use of MCE


Summary

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 IC 50 of 0.1 µM and 1.8 µM, respectively [5] . Tamoxifen Citrate activates autophagy and induces apoptosis [4] .


IC50 & Target

Estrogen receptor

HSP90


In Vitro

Tamoxifen Citrate (ICI 46474) shows strong inhibition of MCF-7 cells (EC 50 =1.41 μM) and to a lesser extent the T47D cells (EC 50 =2.5 μM) but does not affect the MDA-MB-231 cells [2] .

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


In Vivo

The Tamoxifen Citrate-inducible gene knockout strategy has clear advantages in that expression of a gene can be ablated in adult mice at will in a tissue specific manner. To study the role of Med1 in adult heart, 7-week old TmcsMed1 -/- mice are given a daily Iintraperitoneal injection of Tamoxifen Citrate at a dose of 65 mg/kg for 5 days and killed at selected intervals thereafter. qPCR analysis of RNA shows that the Med1 expression begin to decrease after 3 days of Tamoxifen Citrate injection (about 70% decrease), and by 5 days of injection, Med1 expression is almost non-detectable in the heart. Tamoxifen Citrate-inducible cardiac-specific disruption of Med1 (TmcsMed1 -/- ) in adult mice causes dilated cardiomyopathy [3] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00847366 AEterna Zentaris
Non Small Cell Lung Cancer|Solid Tumors|Metastatic Breast Cancer|Sarcomas
May 2008 Not Applicable
NCT02311933 National Cancer Institute (NCI)
Recurrent Breast Carcinoma|Stage III Breast Cancer AJCC v7|Stage IIIA Breast Cancer AJCC v7|Stage IIIB Breast Cancer AJCC v7|Stage IIIC Breast Cancer AJCC v7|Stage IV Breast Cancer AJCC v6 and v7
March 6, 2015 Phase 2
NCT02979301 Mayo Clinic
High Background Uptake on MBI
March 1, 2017 Not Applicable

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

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


Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 88.71 mM ; Need ultrasonic)

Ethanol : 10 mg/mL ( 17.74 mM ; Need ultrasonic)

H 2 O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7742 mL 8.8709 mL 17.7418 mL
5 mM 0.3548 mL 1.7742 mL 3.5484 mL
10 mM 0.1774 mL 0.8871 mL 1.7742 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: corn oil

    Solubility: 10 mg/mL (17.74 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Ethanamine, 2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]-N,N-dimethyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Ethanamine, 2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethyl-, (Z)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Ethanamine, 2-[4-[(1Z)-1,2-diphenyl-1-butenyl]phenoxy]-N,N-dimethyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Tamoxifen citrate
Nolvadex
ICI 46474
Tamoplex
Z-Tamoxifen citrate
Tamox-Puren
Zemide
Kessar
Tamofen
TMX
Tomaxasta
Noltam
Nourytam
I.C.I.46474 citrate
Istubal
Valodex
Soltamox
Genox

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