| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Fluorizoline targets prohibitin 1 (PHB1) and prohibitin 2 (PHB2), which are scaffold proteins involved in mitochondrial function, cell proliferation, and apoptosis. It is a diaryl trifluorothiazoline compound that binds to PHB1/2. Fluorizoline induces apoptosis by upregulating proapoptotic NOXA and BIM proteins.
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| ln Vitro |
In isolated primary CLL cells, fluazoline (1.25–20 μM; 24 hours) causes cell infection [1]. Elevated NOXA protein levels are caused by fluazoline (5–10 μM; 48 hours) [1]. normal B cells and T cells in 24 hours of cells treated with 10 μM fluzoline; counts of normal B cells and T cells in normal CD19+ and CD3+ (48.6% and 82.8% of cells measured after treatment).
In vitro, Fluorizoline reduces the viability of various cancer cell lines with IC50 values ranging from 1.6 μM (Bx-PC3) to 9.4 μM (JeKo-1) at 24 hours. It induces p53-independent apoptosis in various cancer cultures. Fluorizoline upregulates proapoptotic NOXA and BIM mRNAs in wild-type cells, but not in PHBs-depleted cells. It reduces chronic lymphocytic leukemia (CLL) cell viability. |
| ln Vivo |
Fluazoline (15 mg/kg; intraperitoneal; 3 times weekly for 5 weeks) rapidly turned white and showed up in the C57BL/6 Eu-TCL1 mouse CLL model's blood after 3 weeks. An increase in both the overall and CD5+CD19+ CLL cell counts. Cell cancers in the body are not controlled by fluazoline. Splenomegaly indicates that fluazoline does not slow the course of splenic illness [2].
In vivo activity data for Fluorizoline are not extensively documented in publicly available literature. The compound has been studied for its anticancer activity, particularly in leukemia models. Further in vivo studies are needed to fully characterize its antitumor efficacy and therapeutic potential. |
| Enzyme Assay |
The in vitro binding assay for Fluorizoline involves measuring its direct binding to prohibitin 1 (PHB1) and prohibitin 2 (PHB2) proteins. Binding is assessed using surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or pull-down assays. Varying concentrations of Fluorizoline are incubated with recombinant PHB proteins, and binding affinity is determined. Fluorizoline selectively and directly binds to PHB1 and PHB2.
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| Cell Assay |
Apoptosis analysis [1]
Cell Types: Primary CLL cells Tested Concentrations: 1.25 to 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Average EC50 values for strongly reducing cell viability and inducing apoptosis in one dose were 10.9 μM and 19.1 μM, respectively [1]. Dependence method. Western Blot Analysis[1] Cell Types: Primary CLL Cells Tested Concentrations: 5, 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: Resulted in increased NOXA protein levels. In vitro cellular assays for Fluorizoline involve treating various cancer cell lines (e.g., Bx-PC3, JeKo-1, CLL cells) with varying concentrations of the compound. Cell viability is assessed using MTT, CCK-8, or trypan blue exclusion assays. Apoptosis is detected by flow cytometry using Annexin V/PI staining. NOXA and BIM mRNA and protein levels are measured by qRT-PCR and Western blotting. Fluorizoline reduces cell viability with IC50 values of 1.6-9.4 μM and upregulates NOXA and BIM. |
| Animal Protocol |
In vivo animal experiments for Fluorizoline would typically use mouse xenograft models of human cancers, particularly leukemia. Tumor-bearing mice would be administered Fluorizoline via intraperitoneal or oral routes at various doses. Tumor volume would be measured regularly. Apoptosis markers and PHB binding would be assessed in tumor tissues. However, specific in vivo protocols are not extensively documented in public literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of Fluorizoline have not been extensively characterized in publicly available literature. The compound has a molecular weight of 324.32 (C16H11F3N2S). As a small molecule, it is soluble in DMSO and is expected to have reasonable bioavailability. Specific PK parameters including half-life, Cmax, and metabolic pathways are not well documented.
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| Toxicity/Toxicokinetics |
Toxicological data for Fluorizoline are limited in publicly available sources. The compound has been studied in various cancer cell lines, suggesting some level of tolerability. However, systematic toxicology studies including acute, repeated-dose, and genotoxicity assessments have not been well documented. Standard safety pharmacology studies would be required for therapeutic development.
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| References |
[1]. Ana M Cosialls, et al. The prohibitin-binding compound fluorizoline induces apoptosis in chronic lymphocytic leukemia cells through the upregulation of NOXA and synergizes with ibrutinib, 5-aminoimidazole-4-carboxamide riboside or venetoclax. Haematologica. 2017 Sep;102(9):1587-1593.
[2]. Marina Wierz, et al. The prohibitin-binding compound fluorizoline induces apoptosis in chronic lymphocytic leukemia cells ex vivo but fails to prevent leukemia development in a murine model. Haematologica. 2018 Apr;103(4):e154-e157. |
| Additional Infomation |
Fluorizoline (CAS#: 1362243-70-6) is a prohibitin (PHB)-binding compound that selectively binds to PHB1 and PHB2. It induces p53-independent apoptosis in cancer cells by upregulating NOXA and BIM, with IC50 values of 1.6-9.4 μM in various cancer cell lines. Fluorizoline has been studied in leukemia and is not approved for clinical use.
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| Molecular Formula |
C15H8CL2F3NS
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| Molecular Weight |
362.196930885315
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| Exact Mass |
360.97
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| CAS # |
1362243-70-6
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| PubChem CID |
56837157
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
404.6±55.0 °C at 760 mmHg
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| Flash Point |
198.5±31.5 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
5.03
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
446
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(=CC=1)C1(C(N=C(C2C=CC(=CC=2)Cl)S1)(F)F)F
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| InChi Key |
JGDLZQYCDVDWNE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H8Cl2F3NS/c16-11-5-1-9(2-6-11)13-21-15(19,20)14(18,22-13)10-3-7-12(17)8-4-10/h1-8H
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| Chemical Name |
2,5-bis(4-chlorophenyl)-4,4,5-trifluoro-1,3-thiazole
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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 : ~50 mg/mL (~138.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.90 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 25.0 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: 2.5 mg/mL (6.90 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7609 mL | 13.8045 mL | 27.6091 mL | |
| 5 mM | 0.5522 mL | 2.7609 mL | 5.5218 mL | |
| 10 mM | 0.2761 mL | 1.3805 mL | 2.7609 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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