5F-203
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.04%
- No. CAS: 260443-89-8
- Fòrmula: C14H11FN2S
- Peso molecular:258.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-104026
L-KynurenineAryl Hydrocarbon Receptor Agonist -
HY-12684
CH-223191AhR Antagonist -
HY-12451
FICZAhR Agonist -
HY-15001
Stemregenin 1AhR Antagonist -
HY-19317
ITEAryl Hydrocarbon Receptor Agonist -
HY-104026R
L-Kynurenine (Standard)Aryl Hydrocarbon Receptor Agonist -
HY-109044
TapinarofAhR Agonist -
HY-124421R
5F-203 (Standard)Reference Standard -
HY-111278
PyocyaninSecondary Metabolite -
HY-103220
6,2',4'-TrimethoxyflavoneAHR Antagonist -
HY-102023
GNF351AHR Antagonist -
HY-15001G
Stemregenin 1 (GMP)AhR Antagonist
Ver todos los productos específicos de isoformas Cathepsin
MoreVer todos los productos específicos de isoformas Caspase
More
Actividad biológica
Descripciòn
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CYP1A1 |
CYP1B1 |
Cathepsin B |
Caspase 3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-468 | IC50 |
11.17 nM
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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.
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41628058 |
| MDA-MB-453 | IC50 |
25.58 nM
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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.
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41628058 |
| DU-4475 | IC50 |
>500 nM
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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.
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41628058 |
| Hs-578T | IC50 |
>500 nM
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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.
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41628058 |
In Vitro
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].
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468 and T47D
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Concentration:1, 100, 1000 nM
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Incubation Time:24 h
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Result:Induced dose-dependent apoptosis in MDA-MB-468 and T47D cells.
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Cell Line:MDA-MB-468 and T47D
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Concentration:1 μM
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Incubation Time:12 h
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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.
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Cell Line:MDA-MB-468 and T47D
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Concentration:100 nM (MDA-MB-468); 1 μM (T47D)
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Incubation Time:24 h
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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.
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Cell Line:MDA-MB-468
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Concentration:1 μM
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Incubation Time:72 h
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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.
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Cell Line:MDA-MB-468
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Concentration:100 nM
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Incubation Time:24 h
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Result:5F-203-induced expression of proapoptotic BAK-1 and LTA was attenuated in shCYGB cells relative to shGFP cells.
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Cell Line:MDA-MB-468
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Concentration:100 nM
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Incubation Time:24 h
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Result:Silencing CYGB attenuated 5F-203-mediated inhibition of wound healing.
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Cell Line:MDA‑MB‑468, MDA‑MB‑453, DU4475 and Hs578T cells
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Concentration:0.1, 1, 10, 100, 1000 nM
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Incubation Time:72 h
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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.
- RNA extraction experimental
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Protocol For Protein Expression And Purification
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Apoptosis Solutions
- Lysosome and acidic-vesicle live-cell staining
- Genotoxicity/Mutagenicity Study
Chemical Information
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No. CAS 260443-89-8
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Appearance Solid
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Peso molecular 258.32
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Fòrmula C14H11FN2S
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Color Off-white to light yellow
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SMILES
NC1=CC=C(C2=NC3=CC(F)=CC=C3S2)C=C1C
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Synonyms
NSC-703786
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| 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 |
5F-203 Related Classifications
HY-124421 Related Classifications
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