Eganelisib (IPI-549)

製品コードS8330 バッチS833002

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₀H₂₄N₈O₂
	分子量	528.56	CAS No.	1693758-51-8
Solubility (25°C)*	体外	DMSO	100 mg/mL (189.19 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM.
in vitro	Eganelisib (IPI-549) is found to be a remarkably tight binder to PI3K-γ with a Kd of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms. It does not significantly inhibit a panel of 468 mutant and nonmutant protein and lipid kinases (including Class II PI3K isoforms) at 1 μM. In PI3K-α, -β, -γ, and -δ dependent cellular phospho-AKT assays, this compound demonstrates excellent PI3K-γ potency (IC50 = 1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold). Furthermore, it dose dependently inhibits PI3K-γ-dependent bone marrow-derived macrophage (BMDM) migration in vitro. It is also found to be selective against a panel of 80 GPCRs, ion channels, and transporters at 10 μM. In vitro, IPI-549 shows moderate to high cell permeability across Caco-2 cell monolayers, is slowly metabolized in cultured hepatocytes (t1/2 > 360 min), and demonstrates IC50s greater than 20 μM for the CYP isoforms tested (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4).
in vivo	Eganelisib (IPI-549) has excellent oral bioavailability, low clearance, and distributes into tissues with a mean volume of distribution of 1.2 L/kg in vivo (mice, rats, dog, and monkeys). It has a favorable pharmacokinetic profile to allow potent and selective inhibition of PI3K-γ in vivo. This compound can significantly reduce neutrophil migration in a dose-dependent manner in mouse model when administered orally at all of the tested doses. In addition, it has been shown to inhibit tumor growth in murine syngeneic models through alteration of immune cells in the tumor microenvironment.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	SKOV-3 cells
	濃度	--
	反応時間	30 min
	実験の流れ	SKOV-3 cells are seeded into 96-well cell culture-grade plates at a density of 200,000 cells/200 μL/well of RPMI-1640 with 10% FBS. Cells are incubated overnight at 5% CO2 and 37 °C. Eganelisib (IPI-549) is added to the cells, resulting in a final DMSO concentration of 0.5%, and incubated for 30 minutes at 5% CO2 and 37 °C. Media is then aspirated and 50 μL/well of ice-cold lysis buffer is added. Plates are incubated on ice for 5 minutes and then centrifuged at 3000 rpm at 4 °C for 5 minutes.
動物実験	動物モデル	CD-1 mice, Sprague-Dawley rats, beagle dogs and cynomolgus monkeys.
	投薬量	0.5-1.25 mg/mL(For PO dosing); 5-10 mg/mL(for efficacy studies); 0.25-0.4 mg/mL(for IV dosing)
	投与方法	p.o.; i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/27660692/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Immunomodulatory microbubbles targeting integrin αvβ3 in combination with immunotherapy for the theranostic of anaplastic thyroid cancer in mice [ J Control Release, 2025, 387:114189]	PubMed: 40925418
A Phosphatidylinositol 3-Kinase Gamma Inhibitor Enhances Anti-Programmed Death-1/Programmed Death Ligand-1 Antitumor Effects by Remodeling the Tumor Immune Microenvironment of Ovarian Cancer [ MedComm (2020), 2025, 6(8):e70223]	PubMed: 40703194
TRPM2 deficiency contributes to M2b macrophage polarization via the PI3K/AKT/CREB pathway in murine sepsis [ Innate Immun, 2025, 31:17534259251343377]	PubMed: 40405673
VEGFR2 blockade overcomes acquired KRAS G12D inhibitor resistance driven by PI3Kγ activation [ bioRxiv, 2025, 2025.09.16.676456]	PubMed: 41000780
A class I PI3K signalling network regulates primary cilia disassembly in normal physiology and disease [ Nat Commun, 2024, 15(1):7181]	PubMed: 39168978
Adipocyte PI3K links adipostasis with baseline insulin secretion at fasting through an adipoincretin effect [ Cell Rep, 2024, 43(5):114132]	PubMed: 38656871
Combination Treatment Targeting mTOR and MAPK Pathways Has Synergistic Activity in Multiple Myeloma [ Cancers (Basel), 2023, 15(8)2373]	PubMed: 37190302
Pan-PI3K inhibition with copanlisib overcomes Treg- and M2-TAM-mediated immune suppression and promotes anti-tumor immune responses [ Clin Exp Med, 2023, 10.1007/s10238-023-01227-6]	PubMed: 37935952
Inactivation of TRPM7 Kinase Targets AKT Signaling and Cyclooxygenase-2 Expression in Human CML Cells [ Function (Oxf), 2023, 4(6):zqad053]	PubMed: 37786778
Targetable leukemia dependency on noncanonical PI3Kγ signaling [ bioRxiv, 2023, 10.1101/2023.12.15.571909]	PubMed: none

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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