FL-411
Based on 1 Customer Validation
FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1).
For research use only. We do not sell to patients.
- Purity : 99.05%
- CAS No.: 2118944-88-8
- Formula: C18H19N3O2S
- Molecular Weight:341.43
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
BRD4(1) 0.43 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
1.33 μM
Compound: 4l
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Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay
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[PMID: 32153186] |
| MCF7 | IC50 |
1.62 μM
Compound: 9f
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Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
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[PMID: 29172540] |
| MDA-MB-231 | IC50 |
3.27 μM
Compound: 9f
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Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
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[PMID: 29172540] |
In Vitro
FL-411 is a selective BRD4 inhibitor. Binding affinities of FL-411 are measured by TR-FRET against the first and second bromodomains of BRD2(1), BRD4(1), and BRD4(2) with IC50s of 24.60±0.70 μM, 0.47±0.02 μM, 0.93±0.05 μM, respectively. FL-411 possesses a good BRD4(1) inhibition activity (IC50=0.43±0.09 μM), antiproliferative activity (MCF-7, IC50=1.62±0.06 μM; MDA-MB-231, IC50=3.27±0.14 μM), and autophagic activity (42.29% in MCF-7 cells), as well as displays a low toxicity against MCF10A cells). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction and thus activating AMPK-mTOR-ULK1-modulated autophagic pathway in breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2118944-88-8
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Appearance Solid
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Molecular Weight 341.43
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Formula C18H19N3O2S
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Color Yellow to brown
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SMILES
CN1CCC2=C(SC(N=C(C3=CC(C)=C(O)C(C)=C3)N4)=C2C4=O)C1
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Synonyms
BRD4-IN-1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
In Vitro:
DMSO : 5.4 mg/mL (15.82 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, 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.
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.
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 90% (20% SBE-β-CD in Saline)
Solubility: 1.25 mg/mL (3.66 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.54 mg/mL (1.58 mM); Clear solution
This protocol yields a clear solution of ≥ 0.54 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.4 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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (276 KB)
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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)
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Handling Instructions (2659 KB)
References
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, 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 | 2.9289 mL | 14.6443 mL | 29.2886 mL | 73.2215 mL |
| 5 mM | 0.5858 mL | 2.9289 mL | 5.8577 mL | 14.6443 mL | |
| 10 mM | 0.2929 mL | 1.4644 mL | 2.9289 mL | 7.3221 mL | |
| 15 mM | 0.1953 mL | 0.9763 mL | 1.9526 mL | 4.8814 mL |
FL-411 Related Classifications
HY-111102 Related Classifications
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