[CAS NO. 1232221-74-7] APY0201
PRODUCTS SPECIFICATIONS [1232221-74-7]
DESCRIPTION [1232221-74-7]
Overview
| MDL | MFCD28386328 |
|---|---|
| Molecular Weight | 413.48 |
| Molecular Formula | C23H23N7O |
| SMILES | CC1=CC(/C=N/NC2=NC3=CC(C4=CC=NC=C4)=NN3C(N5CCOCC5)=C2)=CC=C1 |
2 Publications Citing Use of MCE
Summary
APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P 2 in the presence of in the presence of [ 33 P]ATP with an IC 50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
IC50 & Target
|
PIKfyve 5.2 nM (IC 50 ) |
IL-12
|
IL-23
|
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 IC 50 s 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.
Appearance
Solid
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
DMSO : ≥ 35 mg/mL ( 84.65 mM )
* "≥" means soluble, but saturation unknown.
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 |