Synonyms: compound 26 [PMID: 27660692] | IPI-549 | IPI549
Compound class:
Synthetic organic
Comment: Eganelisib (IPI549) is an orally bioavailable, highly selective small molecule PI3Kγ inhibitor [1].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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Bioactivity Comments |
IPI549 is >100-fold selective for PI3Kγ over the other lipid and protein kinases tested [1]. In vivo, it robustly inhibits PI3Kγ-mediated neutrophil migration. Cellular IC50s (nM; measuring inhibition of pAKT S473) are 250 (α), 240 (β), 1.2 (γ) and 180 (δ) vs. the four PI3K isozymes in SKOV-3, 786-O, RAW 264.7, and RAJI cells respectively. IPI549 inhibits migration of bone marrow derived macrophages (BMDM) with an IC50 of 85nM in vitro. It inhibits proliferation of mouse MLg2908 lung fibroblasts (IC50 980 nM) [2]. |
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