Cat. No.: HY-W414644

Fluacrypyrim

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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.

For research use only. We do not sell to patients.

Purity: 97.49%
CAS No.: 229977-93-9
Formula: C₂₀H₂₁F₃N₂O₅
Molecular Weight:426.39

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Fluacrypyrim Chemical Structure

CAS No.: 229977-93-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Parasite Isoforms :

All STAT Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	9.8 μM Compound: Fluacrypyrim	Cytotoxicity against human A549 cells assessed as growth inhibition by SRB assay Cytotoxicity against human A549 cells assessed as growth inhibition by SRB assay	[PMID: 23664877]
HL-60	IC₅₀	6.9 μM Compound: Fluacrypyrim	Cytotoxicity against human HL60 cells assessed as growth inhibition by MTT assay Cytotoxicity against human HL60 cells assessed as growth inhibition by MTT assay	[PMID: 23664877]

In Vitro

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 IC₅₀s 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 (PGF_2α) (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 PGF_2α-induced MLC20 phosphorylation in myometrial cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[2]

Cell Line:

HL-60 cells and MDA-MB-231 cells
Concentration:

0, 0.75, 1.5, 3, 6, 12 μM
Incubation Time:

6, 12, 24, 36 h
Result:

Induced G1 arrest in HL-60 cells and MDA-MB-231 cells(24 μM, 48 h)

Real Time qPCR^[1]

Cell Line:

BMNC cells
Concentration:

5 μM
Incubation Time:

10 h
Result:

Downregulated the expression levels of Puma, Bax, and Noxa markedly.

Western Blot Analysis^[1]

Cell Line:

BMNC cells
Concentration:

5 μM
Incubation Time:

4 h
Result:

Downregulated the expression level of protein of p-p53, p53, Puma, Bax, Noxa, and cleaved Caspase-3.

Western Blot Analysis^[2]

Cell Line:

HL-60, K562 and XG-7 cells
Concentration:

0, 0.75, 1.5, 3, 6, 12 μM
Incubation Time:

6, 12, 24, 36 h
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).

In Vivo

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 PGF_2α 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.

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]
Dosage:

20, 50, 75 mg/kg
Administration:

i.p. 3, 24, and 48 h before irradiation
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)

Animal Model:

KM male and female mice (22-28 g)^[3]
Dosage:

50, 100, 200 mg/kg
Administration:

i.p., 1 h before acid injection
Result:

Reduced acetic acid-induced writhing response in mice

Animal Model:

KM male and female mice (22-28 g) and female Sprague Dawley (SD) rats (120-140 g)^[3]
Dosage:

50, 100, 200 mg/kg
Administration:

i.p., 1 h before PGF_2α injection
Result:

Reduced inflammatory activities on mouse and rat swelling models.
Reduced PGF2α-induced pain response.

Chemical Information

CAS No. 229977-93-9
Appearance Solid
Molecular Weight 426.39
Formula C₂₀H₂₁F₃N₂O₅
Color White to off-white
SMILES

COC(/C(C1=C(C=CC=C1)COC2=NC(OC(C)C)=NC(C(F)(F)F)=C2)=C/OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3453 mL

11.7264 mL

23.4527 mL

5 mM

0.4691 mL

2.3453 mL

4.6905 mL

10 mM

0.2345 mL

1.1726 mL

2.3453 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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Fluacrypyrim

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Pyroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Antiparasitic Compound library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Protein-protein Interaction Inhibitor Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

All Parasite Isoforms

All STAT Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Fluacrypyrim Related Classifications

HY-W414644 Related Classifications