Art. -Nr.: HY-124421

5F-203

Name: 5F-203
Brand: MedChemExpress
SKU: HY-124421
Price: 72.00 USD
Availability: InStock
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(Synonyms: NSC-703786)

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5F-203 (NSC-703786) is an aryl hydrocarbon receptor (AhR) agonist and the active moiety of the water-soluble benzothiazole prodrug Phortress (HY-103223). 5F-203 binds to cytosolic AhR and induces CYP1A1 and CYP1B1 expression. 5F-203 activates AhR signaling to induce DNA damage, cell cycle arrest, apoptosis, caspase-3/-7 activation, lysosomal membrane permeabilization, and Cathepsin B release. 5F-203 induces CYGB and pro-apoptotic protein expression and NAG-1 mRNA/protein induction through RNA stabilization. 5F-203 is used in research related to cancers such as triple-negative breast cancer and colorectal cancer.

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Reinheit : 98.04%
CAS. Nr.: 260443-89-8
Formel: C₁₄H₁₁FN₂S
Molecular Weight:258.32

Speicherung:

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

5F-203 Chemical Structure

CAS. Nr.: 260443-89-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]^[2]

CYP1A1

CYP1B1

Cathepsin B

Caspase 3

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Alle Cathepsin Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-468	IC50	11.17 nM	Inhibition of cell growth in parental MDA-MB-468 cells incubated for 72 hrs by Cell Counting Kit-8 assay. Inhibition of cell growth in parental MDA-MB-468 cells incubated for 72 hrs by Cell Counting Kit-8 assay.	41628058
MDA-MB-453	IC50	25.58 nM	Inhibition of cell growth in MDA-MB-453 cells incubated for 72 hrs by Cell Counting Kit-8 assay. Inhibition of cell growth in MDA-MB-453 cells incubated for 72 hrs by Cell Counting Kit-8 assay.	41628058
DU-4475	IC50	>500 nM	Inhibition of cell growth in DU4475 cells incubated for 72 hrs by Cell Counting Kit-8 assay. Inhibition of cell growth in DU4475 cells incubated for 72 hrs by Cell Counting Kit-8 assay.	41628058
Hs-578T	IC50	>500 nM	Inhibition of cell growth in Hs578T cells incubated for 72 hrs by Cell Counting Kit-8 assay. Inhibition of cell growth in Hs578T cells incubated for 72 hrs by Cell Counting Kit-8 assay.	41628058

In Vitro

OthersApoptosisAnti-cancerLysosomal Metabolism

Others

5F-203 is the active moiety of the benzothiazole prodrug Phortress (HY-103223) and undergoes aryl hydrocarbon receptor binding, cytochrome P450 1A1 induction, and DNA adduct formation^[1].
5F-203 effectively induces NAG-1 expression in HCT-116 and MCF-7 cells; it achieves NAG-1 upregulation by enhancing the stability of NAG-1 RNA^[5].

Apoptosis

Anti-cancer

5F-203 (1-1000 nM; 24 h) induces dose-dependent apoptosis in MDA-MB-468 and T47D cells and induces caspase-3/7 activation, a process promoted by CYGB^[2].
5F-203 (1 μM; 72 h) induces CYGB protein expression and pro-apoptotic protein expression in MDA-MB-468 cells, in which GADD45a, LTA, and caspase cleavage are dependent on CYGB^[2].
5F-203 (100 nM; 24 h) induces the expression of pro-apoptotic genes BAK-1, LTA, and GADD45a in MDA-MB-468 cells; it inhibits MDA-MB-468 cell migration, a process associated with CYGB^[2].

Lysosomal Metabolism

Anti-cancer

5F-203 (100 nM-1 μM; 24 h) induces CYGB-dependent lysosomal membrane permeabilization and cathepsin B release in MDA-MB-468 and T47D cells^[2].

Anti-cancer

5F-203 (0.1-1000 nM; 72 h) inhibits the growth of MDA-MB-468 cells with an IC₅₀ of 11.17 nmol/L and inhibits the growth of MDA-MB-453 cells with an IC₅₀ of 25.58 nmol/L, but has no growth inhibitory effect on DU4475 and Hs578T cells, with an IC₅₀ greater than 500 nmol/L^[3].

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

Apoptosis Analysis^[2]

Cell Line:

MDA-MB-468 and T47D
Concentration:

1, 100, 1000 nM
Incubation Time:

24 h
Result:

Induced dose-dependent apoptosis in MDA-MB-468 and T47D cells.

Apoptosis Analysis^[2]

Cell Line:

MDA-MB-468 and T47D
Concentration:

1 μM
Incubation Time:

12 h
Result:

Promoted caspase-3 activation in T47D and MDA-MB-468 cells.
Knockdown of CYGB diminished 5F-203-mediated caspase-3/7 activation.
Enforced expression of CYGB promoted caspase-3/7 activation, and 5F-203 significantly enhanced caspase-3/7 activation in these CYGB-overexpressing cells.

Immunofluorescence^[2]

Cell Line:

MDA-MB-468 and T47D
Concentration:

100 nM (MDA-MB-468); 1 μM (T47D)
Incubation Time:

24 h
Result:

Caused LMP in MDA-MB-468 cells and to a lesser extent in T47D cells. 5F-203-mediated LMP was attenuated in shCYGB MDA-MB-468 cells relative to shGFP MDA-MB-468 cells.\nPromoted cathepsin B release, characterized by diffuse red fluorescent dye staining. 5F-203-mediated cathepsin B release was attenuated in shCYGB MDA-MB-468 cells relative to shGFP MDA-MB-468 cells.

Western Blot Analysis^[2]

Cell Line:

MDA-MB-468
Concentration:

1 μM
Incubation Time:

72 h
Result:

Induced CYGB protein expression.
Induced the expression of proapoptotic proteins BAK-1, GADD45a, and LTA, and caspase-3 cleavage was detected.
CYGB silencing diminished the ability of 5F-203 to induce GADD45a and LTA as well as caspase cleavage, but not BAK-1.

Real Time qPCR^[2]

Cell Line:

MDA-MB-468
Concentration:

100 nM
Incubation Time:

24 h
Result:

5F-203-induced expression of proapoptotic BAK-1 and LTA was attenuated in shCYGB cells relative to shGFP cells.

Cell Migration Assay ^[2]

Cell Line:

MDA-MB-468
Concentration:

100 nM
Incubation Time:

24 h
Result:

Silencing CYGB attenuated 5F-203-mediated inhibition of wound healing.

Cell Viability Assay^[3]

Cell Line:

MDA‑MB‑468, MDA‑MB‑453, DU4475 and Hs578T cells
Concentration:

0.1, 1, 10, 100, 1000 nM
Incubation Time:

72 h
Result:

Inhibited the growth of parental MDA‑MB‑468 cells with an IC₅₀ of 11.17 nmol/L and suppressed the growth of MDA‑MB‑453 cells with an IC₅₀ of 25.58 nmol/L.

Related Protocols :

Chemical Information

CAS. Nr. 260443-89-8
Appearance Solid
Molecular Weight 258.32
Formel C₁₄H₁₁FN₂S
Color Off-white to light yellow
SMILES

NC1=CC=C(C2=NC3=CC(F)=CC=C3S2)C=C1C
Synonyms

NSC-703786
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (387.12 mM; Need ultrasonic; 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

3.8712 mL

19.3558 mL

38.7117 mL

5 mM

0.7742 mL

3.8712 mL

7.7423 mL

10 mM

0.3871 mL

1.9356 mL

3.8712 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.

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 (9.68 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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Peters G, et al. The role of pharmacology in anticancer drug development. ADMET and DMPK. 2018 Mar 25;6(1):4-14.

[2]. Rowland LK, et al. Putative tumor suppressor cytoglobin promotes aryl hydrocarbon receptor ligand-mediated triple negative breast cancer cell death. Journal of cellular biochemistry. 2019 Apr;120(4):6004-6014.

[3]. Ohashi T, et al. ZSTK3744, a Novel Aryl Hydrocarbon Receptor Agonist, Exhibits Efficacy against Chemotherapy-Resistant Triple-Negative Breast Cancer. Cancer research communications. 2026 Feb 01;6(2):421-436. [Content Brief]

[4]. Baek SJ, et al. Changes in gene expression contribute to cancer prevention by COX inhibitors. Progress in lipid research. 2006 Jan;45(1):1-16.

[5]. Eling TE, et al. NSAID activated gene (NAG-1), a modulator of tumorigenesis. Journal of biochemistry and molecular biology. 2006 Nov 30;39(6):649-55.

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	3.8712 mL	19.3558 mL	38.7117 mL	96.7792 mL
	5 mM	0.7742 mL	3.8712 mL	7.7423 mL	19.3558 mL
	10 mM	0.3871 mL	1.9356 mL	3.8712 mL	9.6779 mL
	15 mM	0.2581 mL	1.2904 mL	2.5808 mL	6.4519 mL
	20 mM	0.1936 mL	0.9678 mL	1.9356 mL	4.8390 mL
	25 mM	0.1548 mL	0.7742 mL	1.5485 mL	3.8712 mL
	30 mM	0.1290 mL	0.6452 mL	1.2904 mL	3.2260 mL
	40 mM	0.0968 mL	0.4839 mL	0.9678 mL	2.4195 mL
	50 mM	0.0774 mL	0.3871 mL	0.7742 mL	1.9356 mL
	60 mM	0.0645 mL	0.3226 mL	0.6452 mL	1.6130 mL
	80 mM	0.0484 mL	0.2419 mL	0.4839 mL	1.2097 mL
	100 mM	0.0387 mL	0.1936 mL	0.3871 mL	0.9678 mL

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5F-203

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Alle Cathepsin Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen