1. PI3K/Akt/mTOR
    Immunology/Inflammation
  2. PIKfyve
    Interleukin Related
  3. APY0201

APY0201 

Cat. No.: HY-15982 Purity: >98.0%
Handling Instructions

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.

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

APY0201 Chemical Structure

APY0201 Chemical Structure

CAS No. : 1232221-74-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 708 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target

IC50: 5.2 nM (PIKfyve), 8.4 nM (IL-12p70, in mouse TG-PEC and human PBMC), 16 nM (IL-12p40, in mouse TG-PEC)[1]

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].

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].

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

Molecular Weight

413.48

Formula

C₂₃H₂₃N₇O

CAS No.

1232221-74-7

SMILES

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

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 : ≥ 35 mg/mL (84.65 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (4.84 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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].

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).

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

References
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Keywords:

APY0201APY 0201APY-0201PIKfyveInterleukin RelatedFYVE domain-containing phosphatidylinositol 3-phosphate 5-kinasePhosphatidylinositol 3-phosphate 5-kinaseFab1ILInhibitorinhibitorinhibit

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Product Name:
APY0201
Cat. No.:
HY-15982
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