| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
BRD4 is selectively inhibited by FL-411. Through TR-FRET analysis, FL-411's binding affinity to the first and second bromodomains of BRD2(1), BRD4(1), and BRD4(2) was determined. The IC50 values were 24.60±0.70 μM, 0.47±0.02 μM, and 0.93±0.05 μM, respectively. FL-411 exhibited low toxicity to MCF10A cells and good BRD4(1) inhibitory activity (IC50=0.43±0.09 μM), anti-proliferative 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). By inhibiting the BRD4-AMPK interaction, FL-411 causes ATG5-dependent autophagy-related cell death (ACD) in breast cancer cells by triggering the AMPK-mTOR-ULK1-regulated autophagy pathway [1].
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| ln Vivo |
Two cell line models of breast tumors, MCF-7 and MDA-MB-231, were employed as xenograft models to assess FL-411's in vivo anticancer efficacy. Three distinct FL-411 dosages were used in in vivo experiments: 25 mg/kg, 50 mg/kg, and 100 mg/kg. FL-411 demonstrated a noteworthy and dose-dependent suppression of tumor growth in every model tested; in the MCF-7 and MDA-MB-231 cell models, this inhibition was found to be 80% and 76%, respectively. In every dosage group, a noteworthy decrease in tumor weight was noted (p<0.001). Body weight was not significantly affected by FL-411 in any of the treatment groups. Tumor tissues from control and FL-411-treated mice were processed for LC3 and Ki-67 immunization Histochemical analysis in order to investigate if FL-411-mediated tumor growth suppression in vivo is linked to decreased cell proliferation and increased autophagy-related cell death. enhanced LC3 expression (p<0.001) indicated enhanced autophagy levels following FL-411 treatment, which also markedly decreased the frequency of Ki-67 (p<0.001) positive cells [1].
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| References |
| Molecular Formula |
C18H19N3O2S
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|---|---|
| Molecular Weight |
341.427362680435
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| Exact Mass |
341.119
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| CAS # |
2118944-88-8
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| PubChem CID |
135567026
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
24
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| Complexity |
542
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C2=C(C(NC(C3C=C(C)C(=C(C)C=3)O)=N2)=O)C2=C1CN(C)CC2
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| InChi Key |
PXJZRFLBUBYEPV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19N3O2S/c1-9-6-11(7-10(2)15(9)22)16-19-17(23)14-12-4-5-21(3)8-13(12)24-18(14)20-16/h6-7,22H,4-5,8H2,1-3H3,(H,19,20,23)
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| Chemical Name |
5-(4-hydroxy-3,5-dimethylphenyl)-11-methyl-8-thia-4,6,11-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),5-trien-3-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5.4 mg/mL (~15.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (3.66 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (3.66 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9289 mL | 14.6443 mL | 29.2886 mL | |
| 5 mM | 0.5858 mL | 2.9289 mL | 5.8577 mL | |
| 10 mM | 0.2929 mL | 1.4644 mL | 2.9289 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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