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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-IPI-549
IPI-549

Chemical Structure : IPI-549

CAS No.: 1693758-51-8

IPI-549 (IPI549, Eganelisib)

货号: PC-42233Not For Human Use, Lab Use Only.

Eganelisib (IPI-549) is a potent, highly selective, orally active inhibitor of PI3Kγ with IC50 of 16 nM, displays >100-fold selectivity over other lipid and protein kinases (PI3Kα IC50=3.2 uM, PI3Kβ IC50=3.5 uM, PI3Kδ IC50>8.4 uM).

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

生物&药学活性

Eganelisib (IPI-549) is a potent, highly selective, orally active inhibitor of PI3Kγ with IC50 of 16 nM, displays >100-fold selectivity over other lipid and protein kinases (PI3Kα IC50=3.2 uM, PI3Kβ IC50=3.5 uM, PI3Kδ IC50>8.4 uM).
Eganelisib (IPI-549) demonstrates excellent PI3Kγ potency (IC50=1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold) in cellular phospho-AKT assays, dose dependently inhibits PI3Kγ dependent bone marrow-derived macrophage (BMDM) migration.
Eganelisib (IPI-549) demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo.

物理化学性质&存储条件

分子量 528.564
分子式 C30H24N8O2
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

DMSO: 15 mg/mL

Chemical Name/SMILES

Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 2-amino-N-[(1S)-1-[1,2-dihydro-8-[2-(1-methyl-1H-pyrazol-4-yl)ethynyl]-1-oxo-2-phenyl-3-isoquinolinyl]ethyl]-

参考文献

1. Evans CA, et al. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7.

2. De Henau O, et al. Nature. 2016 Nov 17;539(7629):443-447.

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