Cat. No.: HY-B0005A

Toremifene

(Synonyms: Z-Toremifene; NK 622 free base; FC-1157a free base)

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC₅₀ of 0.07 µM and 2.6 µM, respectively.

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

Purity: 99.73%
CAS No.: 89778-26-7
Formula: C₂₆H₂₈ClNO
Molecular Weight:405.96

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Toremifene Chemical Structure

CAS No.: 89778-26-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All Estrogen Receptor/ERR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	EC₅₀	0.09 μM Compound: toremifene	Inhibition of pseudotyped HIV/EBOV GP infected in human A549 cells assessed as reduction in virus entry measured after 48 hrs by luciferase reporter gene assay Inhibition of pseudotyped HIV/EBOV GP infected in human A549 cells assessed as reduction in virus entry measured after 48 hrs by luciferase reporter gene assay	[PMID: 32490678]
HEK-293T	CC₅₀	17 μM Compound: Tor	Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 38889610]
HEK-293T	EC₅₀	62.8 nM Compound: toremifene	Inhibition of HIV/EBOV GP T519V mutant infected in 293T cells assessed as reduction in virus entry Inhibition of HIV/EBOV GP T519V mutant infected in 293T cells assessed as reduction in virus entry	[PMID: 32490678]
HEK-293T	EC₅₀	62.8 nM Compound: toremifene	Inhibition of HIV/EBOV GP Y517S mutant infected in 293T cells assessed as reduction in virus entry Inhibition of HIV/EBOV GP Y517S mutant infected in 293T cells assessed as reduction in virus entry	[PMID: 32490678]
HeLa	CC₅₀	>100 μM Compound: Toremifene	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay	[PMID: 37021830]
HeLa	EC₅₀	0.67 μM Compound: toremifene	Antiviral activity against Ebola virus 1976 Mayinga infected in human HeLa cells pretreated for 1 hr followed by virus infection measured after 24 hrs by Hoechst staining-based immunofluorescence assay Antiviral activity against Ebola virus 1976 Mayinga infected in human HeLa cells pretreated for 1 hr followed by virus infection measured after 24 hrs by Hoechst staining-based immunofluorescence assay	[PMID: 32490678]
HeLa	EC₅₀	3.25 μM Compound: toremifene	Antiviral activity against Marburg virus Lake Victoria, 2005 Angola infected in human HeLa cells pretreated for 1 hr followed by virus infection measured after 24 hrs by Hoechst staining-based immunofluorescence assay Antiviral activity against Marburg virus Lake Victoria, 2005 Angola infected in human HeLa cells pretreated for 1 hr followed by virus infection measured after 24 hrs by Hoechst staining-based immunofluorescence assay	[PMID: 32490678]
Huh-7	CC₅₀	9.31 μM Compound: 9	Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by cellular ATP method Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by cellular ATP method	[PMID: 35872393]
MCF-10A	IC₅₀	>100 μM Compound: Toremifene	Cytotoxicity against human MCF10A cells by MTT assay Cytotoxicity against human MCF10A cells by MTT assay	[PMID: 31546197]
MCF7	IC₅₀	7 μM Compound: Toremifene	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 31546197]
MDA-MB-231	IC₅₀	13 μM Compound: Toremifene	Antiproliferative activity against human MDA-MB-231 cells by MTT assay Antiproliferative activity against human MDA-MB-231 cells by MTT assay	[PMID: 31546197]
Vero	CC₅₀	10.11 μM Compound: Toremiphene	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	3.58 μM Compound: Toremiphene	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
Vero C1008	IC₅₀	0.162 μM Compound: Toremifene	Antiviral activity against Ebolavirus infected in african green monkey Vero E6 cells assessed as reduction in virus entry after 48 hrs by by Celltiter-Glo luminescent assay Antiviral activity against Ebolavirus infected in african green monkey Vero E6 cells assessed as reduction in virus entry after 48 hrs by by Celltiter-Glo luminescent assay	[PMID: 29272110]
Vero C1008	IC₅₀	0.162 μM Compound: Toremifene	Antiviral activity against Ebolavirus expressing eGFP infected in African green monkey Vero E6 cells assessed as inhibition of viral replication after 48 hrs by spectrofluorometric method Antiviral activity against Ebolavirus expressing eGFP infected in African green monkey Vero E6 cells assessed as inhibition of viral replication after 48 hrs by spectrofluorometric method	[PMID: 29741894]

In Vitro

Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis and other adverse effects resulting from ADT with prostate cancer^[1].
The growth of Ac-1 cells was inhibited by tamoxifen, toremifene and atamestane in vitro with IC50values of 1.8±1.3μM, 1±0.3μM and 60.4±17.2μM, respectively. The combination of toremifene plusatamestane was found to be better than toremifene or atamestane alone in vitro^[3].

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

In Vivo

The effect of this combination was then studied in vivo using Ac-1 xenografts grown in ovariectomized female SCID mice. The mice were injected with toremifene (1000μg/day), atamestane (1000μg/day), tamoxifen (100μg/day), or the combination of toremifene plus atamestane. In this study, our results indicate that the combination of toremifene plus atamestane was as effective as toremifene or tamoxifen alone but may not provide any additional benefit over toremifene alone or tamoxifen alone^[3].

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

Chemical Information

CAS No. 89778-26-7
Appearance Solid
Molecular Weight 405.96
Formula C₂₆H₂₈ClNO
Color White to light yellow
SMILES

ClCC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)\C3=CC=CC=C3
Synonyms

Z-Toremifene; NK 622 free base; FC-1157a free base
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (7)

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Journal Impact Factor

J Med Chem

Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. [Abstract]

2020 Oct 8;63(19):11085-11099. PMID: 32886512
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Viruses

Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]

2021 Jun 28;13(7):1255. PMID: 34203149
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569
Patent

US11696914.
Res Sq

Sex differences in viral entry protein expression, host responses to SARS-CoV-2, and in vitro responses to sex steroid hormone treatment in COVID-19. [Abstract]

2020 Dec 31:rs.3.rs-100914. PMID: 33173861
bioRxiv

2020 May.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (123.16 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4633 mL

12.3165 mL

24.6330 mL

5 mM

0.4927 mL

2.4633 mL

4.9266 mL

10 mM

0.2463 mL

1.2316 mL

2.4633 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (585 KB)
- English - EN (585 KB)
- Français - FR (585 KB)
- Deutsch - DE (585 KB)
- Norwegian - NO (585 KB)
- Español - ES (585 KB)
- Swedish - SV (585 KB)
- Italian - IT (585 KB)
- Portuguese - PT (585 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Matthew R Smith, Selective Estrogen Receptor Modulators to Prevent Treatment-Related Osteoporosis.Rev Urol. 2005; 7(Suppl 3): S30-S35.

[2]. 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]

[3]. Gauri J Sabnis, Luciana Macedo, Olga Goloubeva, Toremifene - Atamestane; Alone or In Combination: Predictions from the Preclinical Intratumoral Aromatase Model. J Steroid Biochem Mol Biol. 2008 January; 108(1-2): 1-7.

[4]. Taneja SS, Morton R, Barnette G, Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene. J Clin Oncol. 2013 Feb 10;31(5):523-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4633 mL	12.3165 mL	24.6330 mL	61.5824 mL
	5 mM	0.4927 mL	2.4633 mL	4.9266 mL	12.3165 mL
	10 mM	0.2463 mL	1.2316 mL	2.4633 mL	6.1582 mL
	15 mM	0.1642 mL	0.8211 mL	1.6422 mL	4.1055 mL
	20 mM	0.1232 mL	0.6158 mL	1.2316 mL	3.0791 mL
	25 mM	0.0985 mL	0.4927 mL	0.9853 mL	2.4633 mL
	30 mM	0.0821 mL	0.4105 mL	0.8211 mL	2.0527 mL
	40 mM	0.0616 mL	0.3079 mL	0.6158 mL	1.5396 mL
	50 mM	0.0493 mL	0.2463 mL	0.4927 mL	1.2316 mL
	60 mM	0.0411 mL	0.2053 mL	0.4105 mL	1.0264 mL
	80 mM	0.0308 mL	0.1540 mL	0.3079 mL	0.7698 mL
	100 mM	0.0246 mL	0.1232 mL	0.2463 mL	0.6158 mL

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Toremifene

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Therapy Drug Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Off-patent Drug Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Toremifene

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Toremifene

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Therapy Drug Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Off-patent Drug Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Toremifene

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Toremifene Related Classifications

Cat. No.: HY-B0005A