IPI-549 is a potent and selective phosphoinositide-3-kinase (PI3K) Inhibitor as an Immuno-Oncology Clinical Candidate (Kd = 0.29 nM). Bioactivity data of IPI-549: biochemcial IC50 (nM) for PI3K isoform: 3200 (); 3500 (); 16 (); and >8400 () respectively. Cellar IC50 (nM) of IPI549 for PI3K isoform: 250 (); 240 (); 1.6 (); and 180 () respectively. IPI-549 shows >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K- mediated neutrophil migration in vivo and is currently in Phase 1 clinical evaluation in subjects with advanced solid tumors.
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