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APY0201

Chemical Structure : APY0201

CAS No.: 1232221-74-7

APY0201 (APY-0201)

Catalog No.: PC-47002Not For Human Use, Lab Use Only.

APY0201 is a potent, highly selective, ATP-competitive PIKfyve inhibitor with IC50 of 5.2 nM, displays broad anti-multiple myeloma activity with EC50 at nanomolar concentrations.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

APY0201 is a potent, highly selective, ATP-competitive PIKfyve inhibitor with IC50 of 5.2 nM, displays broad anti-multiple myeloma activity with EC50 at nanomolar concentrations.
APY0201 interrupts the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3,5)P2.
APY0201 inhibits IL-12/23 production from activated macrophages and monocytes, and demonstrates ameliorated inflammation in an experimental model of colitis.
APY0201 exhibits anti-multiple myeloma activity in cell lines of 100 ex vivo patient-derived primary samples, with increased activity in primary samples harboring trisomies and lacking t(11;14).

Physicochemical Properties

M.Wt 413.48
Formula C23H23N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

>50 mM in DMSO (>20.6 mg/mL)

Chemical Name/SMILES

(E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine

References

1. Hayakawa N, et al. Bioorg Med Chem. 2014 Jun 1;22(11):3021-9.

2. de Campos CB, et al. Haematologica. 2020 Jun;105(6):1641-1649.

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