Fluacrypyrim
Based on 1 Customer Validation
Fluacrypyrim, a Miticide, is a STAT3 inhibitor. Fluacrypyrim significantly increases the protein tyrosine phosphatases(PTPs) activity. Fluacrypyrim inhibits the growth of leukemia cells by a predominant G1 arrest with significant decrease of the protein and mRNA levels of cyclin D1. Fluacrypyrim selectively inhibits STAT3 signaling, inducing growth arrest and apoptosis in STAT3-dependent cancer cells. Fluacrypyrim mitigates IR-induced hematopoietic system injury mainly by preventing apoptosis in the HSCs. Fluacrypyrim demonstrates significant analgesic and anti-inflammatory effects by inhibiting uterine smooth muscle contraction and inflammatory responses.
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- Reinheit: 97.49%
- CAS. Nr.: 229977-93-9
- Formel: C20H21F3N2O5
- Molecular Weight:426.39
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
9.8 μM
Compound: Fluacrypyrim
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Cytotoxicity against human A549 cells assessed as growth inhibition by SRB assay
Cytotoxicity against human A549 cells assessed as growth inhibition by SRB assay
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[PMID: 23664877] |
| HL-60 | IC50 |
6.9 μM
Compound: Fluacrypyrim
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Cytotoxicity against human HL60 cells assessed as growth inhibition by MTT assay
Cytotoxicity against human HL60 cells assessed as growth inhibition by MTT assay
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[PMID: 23664877] |
Fluacrypyrim (FAPM) (3-12 h) reduces the apoptosis rate of BMNCs and its subsets (Lin⁻, Lin⁻c-Kit⁺, LK, and LSK cells) after the 6.5 Gy irradiation[1].
Fluacrypyrim (5 μM, 4-10 h) decreases cell apoptosis by regulating the p53-PUMA pathway in the BMNC cells[1].
Fluacrypyrim (0.1-12 μM, 0-72 h) shows a strong concentration-dependent and time-dependent inhibition of HL-60 cells growth, with an IC50 of 3.8 μM[2].
Fluacrypyrim (1.5-12 μM, 6-36 h) induces G1 arrest of HL-60 cells with downregulation of cyclin-D1[2].
Fluacrypyrim (0.75-12 μM, 6-36 h) significantly inhibits constitutive phosphotyrosine levels of STAT3 (tyr705) in HL-60 cells, an effect that can be reversed by sodium pervanadate treatment[2].
Fluacrypyrim (0.75-12 μM, 12 h) induces a dose-dependent increase of tyrosine phosphatase activity in HL-60 cells[2].
Fluacrypyrim (3-12 μM, 8-24 h) significantly inhibits STAT3-dependent luciferase activity in both IL-6-stimulated HepG-2 cells and c-Src-transfected NIH 3T3 cells[2].
Fluacrypyrim (0.75-12 μM, 24 h) suppresses constitutively active STAT3, thereby blocking cyclin D1 and c-Myc expression in HL-60 cells[2].
Fluacrypyrim (0.75-12 μM, 24 h) preferentially suppresses growth of cancer cells harboring constitutively active STAT3, with IC50 s of 3.8 μM (HL-60 cells), 6.0 μM (K562 cells), 8.2 μM (XG-7 cells) and 12.3 μM (Jurkat-T cells)[2].
Fluacrypyrim (6-24 μM, 24 h) induces caspase-dependent apoptosis in breast carcinoma cells (MDA-MB-231 cells) that harbor constitutively activated STAT3[2].
Fluacrypyrim (0.62-10 μM, 60 min) significantly inhibits uterine contractions induced by Dinoprost (PGF2α) (HY-12956), Oxytocin (HY-17571), acetylcholine (Ach) and KCl in a dose-dependent manner (pD2 values ranging from 5.72 to 5.92)[3].
Fluacrypyrim (2.5-10 μM) inhibits PGF2α-induced MLC20 phosphorylation in myometrial cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 cells and MDA-MB-231 cells
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Concentration:0, 0.75, 1.5, 3, 6, 12 μM
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Incubation Time:6, 12, 24, 36 h
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Result:Induced G1 arrest in HL-60 cells and MDA-MB-231 cells(24 μM, 48 h)
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Cell Line:BMNC cells
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Concentration:5 μM
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Incubation Time:10 h
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Result:Downregulated the expression levels of Puma, Bax, and Noxa markedly.
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Cell Line:BMNC cells
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Concentration:5 μM
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Incubation Time:4 h
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Result:Downregulated the expression level of protein of p-p53, p53, Puma, Bax, Noxa, and cleaved Caspase-3.
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Cell Line:HL-60, K562 and XG-7 cells
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Concentration:0, 0.75, 1.5, 3, 6, 12 μM
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Incubation Time:6, 12, 24, 36 h
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Result:Decreased the level of pRb (ser807/881) in HL-60 cells (3, 6, 12 μM).
Reduced the expression of cyclin D3 and CDK4 slightly and significantly only in the higher concentrations in HL-60 cells (3, 6, 12 μM).
Decreased the cyclin D1 expression dose-dependently in HL-60 cells (3, 6, 12 μM).
Decreased the STAT3 tyr705 phosphorylation without affecting STAT3 ser727 phosphorylation and total STAT3 protein level in HL-60, K562 and XG-7 cells (0, 0.75, 1.5, 3, 6, 12 μM).
Reduced the expression of STAT5 only at the highest concentration and showed no alteration on STAT1 in HL-60 cells (0, 0.75, 1.5, 3, 6, 12 μM).
Fluacrypyrim (20-75 mg/kg, i.p., 3-48 h before irradiation, single dose) mitigates IR-induced hematopoietic system injury in the C57BL/6J (CD45.2) mice and B6.SJL/BoyJ (CD45.1) mice[1].
Fluacrypyrim (50-200 mg/kg, i.p., 1 h before acid injection, single dose) reduces Acetic acid (HY-Y0319)-induced writhing response in mice[3].
Fluacrypyrim (100-200 mg/kg, i.p., 1 h before PGF2α injection, single dose) reduces inflammatory activities and pain response on mouse and rat swelling models[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The male C57BL/6J (CD45.2) mice and male B6.SJL/BoyJ (CD45.1) mice(6-8 weeks) were subjected to either a sublethal dose (6.5 Gy) or lethal dose (8.0, 8.5, 9.0 Gy) of total body irradiation (TBI) using a 60Co γ-ray source at a dose rate of approximately 62 cGy/min[1]
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Dosage:20, 50, 75 mg/kg
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Administration:i.p. 3, 24, and 48 h before irradiation
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Result:Ameliorated pancytopenia in the mice subjected to irradiation (20, 50, 75 mg/kg) (6.5 Gy).
Improved the survival rate of mice after lethal irradiation(50 mg/kg) (8.0 Gy, 8.5 Gy, 9.0 Gy).
Alleviated irradiation-induced injury to BM (6.5 Gy).
Accelerated the recovery of HSPCs after irradiation exposure (6.5 Gy).
Enhanced the self-renewal capacity of HSCs after irradiation (CD45.2: 6.5 Gy) (CD45.1: 9.0 Gy)
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Animal Model:KM male and female mice (22-28 g)[3]
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Dosage:50, 100, 200 mg/kg
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Administration:i.p., 1 h before acid injection
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Result:Reduced acetic acid-induced writhing response in mice
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Animal Model:KM male and female mice (22-28 g) and female Sprague Dawley (SD) rats (120-140 g)[3]
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Dosage:50, 100, 200 mg/kg
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Administration:i.p., 1 h before PGF2α injection
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Result:Reduced inflammatory activities on mouse and rat swelling models.
Reduced PGF2α-induced pain response.
Chemical Information
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CAS. Nr. 229977-93-9
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Appearance Solid
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Molecular Weight 426.39
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Formel C20H21F3N2O5
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Color White to off-white
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SMILES
COC(/C(C1=C(C=CC=C1)COC2=NC(OC(C)C)=NC(C(F)(F)F)=C2)=C/OC)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (234.53 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.86 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.86 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (25.0 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.
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.
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Korean - KR (458 KB)
- Portuguese - PT (458 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Zhang X, et al. Fluacrypyrim Protects Hematopoietic Stem and Progenitor Cells against Irradiation via Apoptosis Prevention. Molecules. 2024 Feb 9;29(4):816. [Content Brief]
[2]. Yu ZY, et al. Fluacrypyrim, a novel STAT3 activation inhibitor, induces cell cycle arrest and apoptosis in cancer cells harboring constitutively-active STAT3. Int J Cancer. 2010 Sep 1;127(6):1259-70. [Content Brief]
[3]. Li Z, et al. Flucrypyrim, a novel uterine relaxant, has antinociceptive and anti-inflammatory effects in vivo. Sci Rep. 2017 Feb 21;7:42040. [Content Brief]
[4]. Sakuda S, et al. Inhibitory effects of respiration inhibitors on aflatoxin production. Toxins (Basel). 2014 Mar 26;6(4):1193-200. [Content Brief]
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 | 2.3453 mL | 11.7264 mL | 23.4527 mL | 58.6318 mL |
| 5 mM | 0.4691 mL | 2.3453 mL | 4.6905 mL | 11.7264 mL | |
| 10 mM | 0.2345 mL | 1.1726 mL | 2.3453 mL | 5.8632 mL | |
| 15 mM | 0.1564 mL | 0.7818 mL | 1.5635 mL | 3.9088 mL | |
| 20 mM | 0.1173 mL | 0.5863 mL | 1.1726 mL | 2.9316 mL | |
| 25 mM | 0.0938 mL | 0.4691 mL | 0.9381 mL | 2.3453 mL | |
| 30 mM | 0.0782 mL | 0.3909 mL | 0.7818 mL | 1.9544 mL | |
| 40 mM | 0.0586 mL | 0.2932 mL | 0.5863 mL | 1.4658 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4691 mL | 1.1726 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3909 mL | 0.9772 mL | |
| 80 mM | 0.0293 mL | 0.1466 mL | 0.2932 mL | 0.7329 mL | |
| 100 mM | 0.0235 mL | 0.1173 mL | 0.2345 mL | 0.5863 mL |
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