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Eganelisib

MCE 国际站：Eganelisib

产品活性：Eganelisib (IPI549) 是一种有效的选择性 PI3Kγ 抑制剂，IC₅₀ 为 16 nM，选择性比其他脂类和蛋白质激酶高出 100 多倍。

作用靶点：PI3K

In Vitro: Eganelisib (IPI549) inhibits PI3Kγ with IC₅₀ of 16 nM, with >100-fold selectivity over other lipid and protein kinases (PI3Kα IC₅₀=3.2 µM, PI3Kβ IC₅₀=3.5 µM, PI3Kδ IC₅₀>8.4 µM). Eganelisib is evaluated for activity across all Class I PI3K isoforms. The binding affinity of Eganelisib for PI3K-γ is determined by measuring the individual rates constants and for PI3K-α, β and δ using equilibrium fluorescent titration. Eganelisib is a remarkably tight binder to PI3Kγ with a K_d of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms (PI3Kα K_d=17 nM, PI3Kβ K_d=82 nM, PI3Kδ K_d=23 M). In PI3K-α, -β, -γ, and -δ dependent cellular phospho-AKT assays, Eganelisib demonstrates excellent PI3K-γ potency (IC₅₀=1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold). Cellular IC₅₀s for Class I PI3Kα (250 nM), PI3Kβ (240 nM), PI3Kγ (1.2 nM), PI3Kδ (180 nM) are determined in SKOV-3, 786-O, RAW 264.7, and RAJI cells, respectively, by monitoring inhibition of pAKT S473 by ELISA. Furthermore, Eganelisib dose dependently inhibits PI3Kγ dependent bone marrow-derived macrophage (BMDM) migration. Eganelisib is selective against a panel of 80 GPCRs, ion channels, and transporters at 10 µM.

In Vivo: Eganelisib (IPI549) demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration. In vivo (mice, rats, dog, and monkeys), Eganelisib has excellent oral bioavailability, low clearance, and distributed into tissues with a mean volume of distribution of 1.2 L/kg. Overall, Eganelisib has a favorable pharmacokinetic profile to allow potent and selective inhibition of PI3K-γ in vivo. The t_1/2 of IPI-549 for mouse, rat, dog and monkey is 3.2, 4.4, 6.7 and 4.3 h, respectively. Eganelisib significantly reduces neutrophil migration in a dose dependent manner in this model when administered orally at all of the tested doses.

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