Art. -Nr.: HY-15982

APY0201

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P₂ in the presence of in the presence of [³³P]ATP with an IC₅₀ of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.

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Reinheit: 99.42%
CAS. Nr.: 1232221-74-7
Formel: C₂₃H₂₃N₇O
Molecular Weight:413.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

APY0201 Chemical Structure

CAS. Nr.: 1232221-74-7

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PIKfyve

5.2 nM (IC₅₀)

IL-12

IL-23

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

In Vitro

APY0201 works differently from anti-IL-12/23 antibodies and acts by inhibiting production of these proinflammatory cytokines with characteristic selectivity over other cytokines, including tumor necrosis factor-alpha (TNF-α). In stimulated thioglycollate-induced mouse peritoneal exudate cells (TG-PEC), APY0201 strongly inhibits IL-12p70 and IL-12p40 production, with IC₅₀s of 8.4 and 16 nM, respectively. APY0201 also inhibits IL-12p40 at 99 nM in human PBMC. APY0201 shows significant selectivity for the production of IL-12p70 and IL-12p40 over TNF-α, and this selectivity is maintained across species^[1].

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

In Vivo

Oral APY0201 at a 30 mg/kg dose shows significant reduction of IL-12p70 production (78% inhibition relative to that of the vehicle control), which implys that the inhibitory potential of APY0201 against IL-12 is confirmed in the animal experiment^[1].

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

Chemical Information

CAS. Nr. 1232221-74-7
Appearance Solid
Molecular Weight 413.48
Formel C₂₃H₂₃N₇O
Color Light yellow to yellow
SMILES

CC1=CC(/C=N/NC2=NC3=CC(C4=CC=NC=C4)=NN3C(N5CCOCC5)=C2)=CC=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

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Journal Impact Factor

Cancer Res

Concurrent Inhibition of the RAS-MAPK Pathway and PIKfyve Is a Therapeutic Strategy for Pancreatic Cancer. [Abstract]

2025 Apr 15;85(8):1479-1495. PMID: 39932818
Phytomedicine

Targeting GRB2 with Polyphyllin H overcomes PIKFYVE inhibitor resistance in bladder cancer by blocking Akt-SREBP1-SCD1 pathway. [Abstract]

2026 May:154:158011. PMID: 41795291
eGastroenterology

Phosphoinositide kinase PIKfyve inhibitor apilimod blocks hepatitis E virus infection. [Abstract]

2026 Mar 31;4(1):e100348. PMID: 41948149
Haematologica

Identification of PIKfyve kinase as a target in multiple myeloma. [Abstract]

2020 Jun;105(6):1641-1649. PMID: 31582538
University of North Carolina at Chapel Hill

2024.
J Oncol

APY0201 Represses Tumor Growth through Inhibiting Autophagy in Gastric Cancer Cells. [Abstract]

2022 Jun 24:2022:7104592. PMID: 36245991

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 35 mg/mL (84.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.4185 mL

12.0925 mL

24.1850 mL

5 mM

0.4837 mL

2.4185 mL

4.8370 mL

10 mM

0.2418 mL

1.2092 mL

2.4185 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (4.84 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 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 (20.0 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 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 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

Protokoll

Cell Assay^[1]

Mouse TG-PEC or human PBMC are incubated with APY0201 (1, 10, 100, 1000 and 10⁴ nM) in the presence of 100 ng/mL mouse or human IFN-γ and 0.05%w/v Staphylococcus aureus Cowan I strain (SAC)^[1].

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

Animal Administration^[1]

Mice^[1]
Female BALB/c mice (n=3) are used. Blood samples (systemic) or from the portal vein (portal) under anesthesia. After 30 min, mice are anesthetized with diethyl ether, and blood samples are collected by cardiacpuncture. Blood is collected in tubes containing 0.5 M-EDTA solution (pH 8.0).

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (583 KB)
- English - EN (583 KB)
- Français - FR (583 KB)
- Deutsch - DE (583 KB)
- Norwegian - NO (583 KB)
- Español - ES (583 KB)
- Swedish - SV (583 KB)
- Italian - IT (583 KB)
- Korean - KR (583 KB)
- Portuguese - PT (583 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)

Verweise

[1]. Hayakawa N, et al. Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201. Bioorg Med Chem. 2014 Jun 1;22(11):3021-9. [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, 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	2.4185 mL	12.0925 mL	24.1850 mL	60.4624 mL
	5 mM	0.4837 mL	2.4185 mL	4.8370 mL	12.0925 mL
	10 mM	0.2418 mL	1.2092 mL	2.4185 mL	6.0462 mL
	15 mM	0.1612 mL	0.8062 mL	1.6123 mL	4.0308 mL
	20 mM	0.1209 mL	0.6046 mL	1.2092 mL	3.0231 mL
	25 mM	0.0967 mL	0.4837 mL	0.9674 mL	2.4185 mL
	30 mM	0.0806 mL	0.4031 mL	0.8062 mL	2.0154 mL
	40 mM	0.0605 mL	0.3023 mL	0.6046 mL	1.5116 mL
	50 mM	0.0484 mL	0.2418 mL	0.4837 mL	1.2092 mL
	60 mM	0.0403 mL	0.2015 mL	0.4031 mL	1.0077 mL
	80 mM	0.0302 mL	0.1512 mL	0.3023 mL	0.7558 mL

Keywords

APY0201

6 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) APY0201

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APY0201 Related Classifications

HY-15982 Related Classifications