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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PIKfyve-APY0201
APY0201

Chemical Structure : APY0201

CAS No.: 1232221-74-7

APY0201 (APY-0201)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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).

物理化学性质&存储条件

分子量 413.48
分子式 C23H23N7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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