Art. -Nr.: HY-14586

Irosustat

(Synonyms: STX64; BN83495; 667-Coumate)

1 Cited Publications

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Irosustat is a potent steroid sulfatase inhibitor, with an IC₅₀ of 8 nM, and exhibits anti-breast cancer activity.

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Reinheit: 99.72%
CAS. Nr.: 288628-05-7
Formel: C₁₄H₁₅NO₅S
Molecular Weight:309.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Irosustat Chemical Structure

CAS. Nr.: 288628-05-7

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Irosustat is a potent steroid sulfatase inhibitor, with an IC₅₀ of 8 nM, and exhibits anti-breast cancer activity.

IC₅₀ & Target

IC50: 8 nM (Steroid sulfatase)^[1], 0.2 nM (Steroid sulfatase, MCF-7 cells)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
JEG-3	IC₅₀	0.421 μM Compound: STX64	Inhibition of steroid sulfatase in human JEG-3 cells assessed as [14C]-Estrone formation using [3H]E1S as substrate Inhibition of steroid sulfatase in human JEG-3 cells assessed as [14C]-Estrone formation using [3H]E1S as substrate	[PMID: 27143133]
JEG-3	IC₅₀	1.5 nM Compound: 1, STX64, BN83495	Inhibition of steroid sulfatase in human JEG3 cells by scintillation spectrometry Inhibition of steroid sulfatase in human JEG3 cells by scintillation spectrometry	[PMID: 20148564]
JEG-3	IC₅₀	1.5 nM Compound: STX64	Inhibition of steroid sulfatase activity in human JEG3 cells Inhibition of steroid sulfatase activity in human JEG3 cells	[PMID: 18590272]
JEG-3	IC₅₀	1.5 nM Compound: STX64, 667COUMATE, BN83495	Inhibition of steroid sulfatase in JEG3 cell membrane Inhibition of steroid sulfatase in JEG3 cell membrane	[PMID: 17580845]
JEG-3	IC₅₀	2.1 nM Compound: STX-64; BN83495	Inhibition of steroid sulfatase in human JEG3 cells using [3H] E1S as substrate incubated for 20 hrs by scintillation spectrometry analysis Inhibition of steroid sulfatase in human JEG3 cells using [3H] E1S as substrate incubated for 20 hrs by scintillation spectrometry analysis	[PMID: 32173116]
JEG-3	IC₅₀	300 nM Compound: 1, STX64, BN83495	Inhibition of aromatase in human JEG3 cells by scintillation spectrometry Inhibition of aromatase in human JEG3 cells by scintillation spectrometry	[PMID: 20148564]
JEG-3	IC₅₀	300 nM Compound: STX64	Inhibition of aromatase activity in human JEG3 cells Inhibition of aromatase activity in human JEG3 cells	[PMID: 18590272]
JEG-3	IC₅₀	6.4 nM Compound: STX-64; BN83495	Inhibition of steroid sulfatase in human JEG3 cell lysates using [3H] E1S as substrate after 1 hr by scintillation spectrometry analysis Inhibition of steroid sulfatase in human JEG3 cell lysates using [3H] E1S as substrate after 1 hr by scintillation spectrometry analysis	[PMID: 32173116]
MCF7	IC₅₀	350 nM Compound: 1, 667-Coumate	Irreversible inhibition of steroid sulfatase in human intact MCF7 cells Irreversible inhibition of steroid sulfatase in human intact MCF7 cells	[PMID: 22264754]
MCF7	IC₅₀	350 nM Compound: 3, 667-Coumate	Inhibition of steroid sulfatase in human intact MCF7 cells Inhibition of steroid sulfatase in human intact MCF7 cells	[PMID: 21925885]
RAW264.7	IC₅₀	81.04 nM Compound: STX-64, BN83495	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS-challenge measured after 24 hrs by EIA Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS-challenge measured after 24 hrs by EIA	[PMID: 24360561]
RAW264.7	IC₅₀	85.76 μM Compound: STX-64, BN83495	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production administered 1 hr prior to LPS-challenge measured after 24 hrs by Griess assay Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production administered 1 hr prior to LPS-challenge measured after 24 hrs by Griess assay	[PMID: 24360561]
T47D	IC₅₀	0.92 μM Compound: STX-64; BN83495	Antiproliferative activity against human T47D cells assessed as reduction in cell proliferation measured after 5 days in presence of estradiol sulfate by crystal violet staining based assay Antiproliferative activity against human T47D cells assessed as reduction in cell proliferation measured after 5 days in presence of estradiol sulfate by crystal violet staining based assay	[PMID: 32173116]

In Vitro

Irosustat (667 COUMATE) is a potent steroid sulfatase inhibitor, with an IC₅₀ of 8 nM^[1]. Irosustat (667 COUMATE) inhibits steroid sulphatase (STS) activity in MCF-7 cells with an IC₅₀ of 0.2 nM, but has no effect on the morphology or proliferation of MCF-7 cells at 10 μM^[2].

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

In Vivo

Irosustat potently inhibits rat liver, with inhibition of >90% when at a 1 mg/kg concentration. Irosustat (2 mg/kg, p.o. for 5 d) blocks the uterine growth stimulated by oestrone sulfate (E1S) in ovariectomized rats. In addition, Irosustat (2, 10 mg/kg, p.o.) plus E1S dose-dependently decreases the growth of NMU-induced mammary tumors in ovariectomized rats^[1]. Irosustat (667 COUMATE; 10 mg/kg, p.o.) shows 97.9 ± 0.06% inhibition on steroid sulphatase (STS) activity in rat liver^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 288628-05-7
Appearance Solid
Molecular Weight 309.34
Formel C₁₄H₁₅NO₅S
Color White to off-white
SMILES

O=C1OC2=CC(OS(=O)(N)=O)=CC=C2C3=C1CCCCC3
Synonyms

STX64; BN83495; 667-Coumate
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Mol Cell Endocrinol

Bisphenol A-sulfate conjugate disrupts AURKA transcription and cell cycle in BeWo cytotrophoblasts. [Abstract]

2022 Apr 5:545:111561. PMID: 35041905

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (323.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

3.2327 mL

16.1634 mL

32.3269 mL

5 mM

0.6465 mL

3.2327 mL

6.4654 mL

10 mM

0.3233 mL

1.6163 mL

3.2327 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 25 mg/mL (80.82 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 20% SBE-β-CD in Saline

Solubility: 2 mg/mL (6.47 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

MCF-7 cells are cultured in growth medium (minimum essential medium (MEM) containing, phenol red, 10% foetal calf serum (FCS) and essential nutrients). When the cells reach 60% confluency, they are treated with Irosustat (0.001-10 μM) in growth medium. After 72 h of incubation, photographs are taken under normal conditions of light and the number of attached cells in each flask is determined using a Coulter cell counter^[2].

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

Animal Administration^[1]

Rats^[1]
Ludwig rats bearing mammary tumors are used in the assay. Tumor development is monitored, and animals are ovariectomized when tumors reach 0.8-1.5 cm in diameter. Tumors are allowed to regress over a 12- to 13-day period to confirm their hormone-dependent status. Regrowth of tumors is stimulated with oestrone sulfate (E1S; 50 μg/day, s.c.). When tumors have regrown, animals continue to receive either E1S alone or E1S plus Irosustat at 10 mg/kg/day or 2 mg/kg/day, p.o., until tumor regression has occurred. Tumor volumes are calculated from two measured diameters^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)

Verweise

[1]. Purohit A, et al. In vivo inhibition of estrone sulfatase activity and growth of nitrosomethylurea-induced mammary tumors by 667 COUMATE. Cancer Res. 2000 Jul 1;60(13):3394-6. [Content Brief]

[2]. Raobaikady B, et al. Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2-methoxyoestradiol-bis-sulphamate. J Steroid Biochem Mol Biol. 2003 Feb;84(2-3):351-8. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2327 mL	16.1634 mL	32.3269 mL	80.8172 mL
	5 mM	0.6465 mL	3.2327 mL	6.4654 mL	16.1634 mL
	10 mM	0.3233 mL	1.6163 mL	3.2327 mL	8.0817 mL
	15 mM	0.2155 mL	1.0776 mL	2.1551 mL	5.3878 mL
	20 mM	0.1616 mL	0.8082 mL	1.6163 mL	4.0409 mL
	25 mM	0.1293 mL	0.6465 mL	1.2931 mL	3.2327 mL
	30 mM	0.1078 mL	0.5388 mL	1.0776 mL	2.6939 mL
	40 mM	0.0808 mL	0.4041 mL	0.8082 mL	2.0204 mL
	50 mM	0.0647 mL	0.3233 mL	0.6465 mL	1.6163 mL
	60 mM	0.0539 mL	0.2694 mL	0.5388 mL	1.3470 mL
	80 mM	0.0404 mL	0.2020 mL	0.4041 mL	1.0102 mL
	100 mM	0.0323 mL	0.1616 mL	0.3233 mL	0.8082 mL

Keywords

Irosustat

1 Cited Publications

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Irosustat

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Breast Cancer Compound Library

Targeted Diversity Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Irosustat

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Irosustat

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Breast Cancer Compound Library

Targeted Diversity Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Irosustat

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Irosustat Related Classifications

HY-14586 Related Classifications