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Eganelisib (IPI-549)

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.

Eganelisib (IPI-549)化学構造

CAS No. 1693758-51-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 59500 国内在庫あり
JPY 142000 国内在庫あり
JPY 595500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Eganelisib (IPI-549)関連製品

シグナル伝達経路

PI3K Signaling Pathways

PI3Kシグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
RAW264.7 Function assay 30 mins Inhibition of PI3Kgamma in C5a-stimulated mouse RAW264.7 cells assessed as reduction in AKT phosphorylation at S473 incubated for 30 mins followed by stimulation with C5a for 3 mins by ELISA, IC50 = 0.0012 μM. 27660692
Sf9 Function assay 15 mins Inhibition of human recombinant full length N-terminal His-tagged PI3Kgamma expressed in Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo luminescence assay, IC50 = 0.016 μM. 27660692
Raji Function assay 30 mins Inhibition of PI3Kdelta in IgM-stimulated human Raji cells assessed as reduction in AKT phosphorylation at S473 incubated for 30 mins followed by stimulation with IgM for 30 mins by ELISA, IC50 = 0.18 μM. 27660692
786-O Function assay 30 mins Inhibition of PI3Kbeta in human 786-O cells assessed as reduction in AKT phosphorylation at S473 after 30 mins by ELISA, IC50 = 0.24 μM. 27660692
SKOV-3 Function assay 30 mins Inhibition of PI3Kalpha in human SKOV-3 cells assessed as reduction in AKT phosphorylation at S473 after 30 mins by ELISA, IC50 = 0.25 μM. 27660692
Sf9 Function assay 15 mins Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110alpha/p85alpha coexpressed in baculovirus infected Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo, IC50 = 3.2 μM. 27660692
Sf9 Function assay 15 mins Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110beta/p85alpha coexpressed in baculovirus infected Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo , IC50 = 3.5 μM. 27660692
Sf9 Function assay Binding affinity to human recombinant full length N-terminal His-tagged PI3Kgamma expressed in Sf9 insect cells by equilibrium fluorescence titration analysis, Kd = 0.00029 μM. 27660692
Sf9 Function assay Binding affinity to human recombinant full length N-terminal His6-tagged PI3K p110alpha/p85alpha coexpressed in baculovirus infected Sf9 insect cells by equilibrium fluorescence titration analysis, Kd = 0.017 μM. 27660692
Sf9 Function assay Binding affinity to human recombinant full length N-terminal GST-tagged PI3K p110delta/p85alpha coexpressed in baculovirus infected Sf9 insect cells by equilibrium fluorescence titration analysis, Kd = 0.023 μM. 27660692
Sf9 Function assay Binding affinity to human recombinant full length N-terminal His6-tagged PI3K p110beta/p85alpha coexpressed in baculovirus infected Sf9 insect cells by equilibrium fluorescence titration analysis, Kd = 0.082 μM. 27660692
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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.
Targets
PI3Kγ [1]
(Cell-free assay)
16 nM
In Vitro
In vitro 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, IPI-549 demonstrates excellent PI3K-γ potency (IC50 = 1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold). Furthermore, IPI-549 dose dependently inhibits PI3K-γ-dependent bone marrow-derived macrophage (BMDM) migration in vitro. IPI-549 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)[1].
細胞実験 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. Compounds are 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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-AKT / AKT / p-p65 / p65 27642729
In Vivo
In Vivo In vivo (mice, rats, dog, and monkeys), IPI-549 has excellent oral bioavailability, low clearance, and distributes into tissues with a mean volume of distribution of 1.2 L/kg. It has a favorable pharmacokinetic profile to allow potent and selective inhibition of PI3K-γ in vivo. IPI-549 can significantly reduce neutrophil migration in a dose-dependent manner in mouse model when administered orally at all of the tested doses. In addition, IPI-54 has been shown to inhibit tumor growth in murine syngeneic models through alteration of immune cells in the tumor microenvironment[1].
動物実験 動物モデル CD-1 mice, Sprague-Dawley rats, beagle dogs and cynomolgus monkeys.
投与量 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)
投与経路 p.o.; i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03980041 Completed
Bladder Cancer|Urothelial Carcinoma|Solid Tumor|Advanced Cancer
Infinity Pharmaceuticals Inc.|Bristol-Myers Squibb
 September 25 2019 Phase 2
NCT02637531 Active not recruiting
Advanced Solid Tumors (Part A/B/C/D)|Non-small Cell Lung Cancer (Part E)|Melanoma (Part E)|Squamous Cell Cancer of the Head and Neck (Part E)|Triple Negative Breast Cancer (Part F)|Adrenocortical Carcinoma (Part G)|Mesothelioma (Part G)|High-circulating Myeloid-derived Suppressor Cells (Part H)
Infinity Pharmaceuticals Inc.
 December 2015 Phase 1

化学情報

分子量 528.56 化学式

C30H24N8O2
CAS No. 1693758-51-8 SDF Download Eganelisib (IPI-549) SDFをダウンロードする
Smiles CC(C1=CC2=C(C(=CC=C2)C#CC3=CN(N=C3)C)C(=O)N1C4=CC=CC=C4)NC(=O)C5=C6N=CC=CN6N=C5N
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (189.19 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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