IC-87114

製品コードS1268 バッチS126801

印刷

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

C₂₂H₁₉N₇O

分子量

397.43

CAS No.

371242-69-2

Solubility (25°C)*

体外

4-Methylpyridine (warmed with 50ºC water bath)

10 mg/mL (25.16 mM)

DMSO

0.66 mg/mL (1.66 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

4%DMSO 1 30%PEG300 2 66%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

0.700mg/ml (1.76mM)

Taking the 1 mL working solution as an example, add 40 μL of 17.5 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	IC-87114は、無細胞アッセイにおいてIC50が0.5 µMの選択的PI3Kδ阻害剤であり、PI3Kγよりも58倍、PI3Kα/βよりも100倍以上選択性が高いです。
in vitro	IC-87114 selectively inhibits PI3Kδ and not sensitive to PI3Kα, β, and γ. In human neutrophils, IC87114 (5 µM) potently inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-stimulated phosphatidylinositol triphosphate (PIP3) biosynthesis and chemotaxis. IC87114 (5 µM) also inhibits polarized morphology and spreading of neutrophils. In human acute myeloid leukemia (AML) blast cells, such as bone marrow mononuclear cells (BMMCs), IC87114 (10 µM) inhibits both constitutive and Flt-3-stimulated Akt phosphorylation and cell proliferation. It is also found that IC87114 (5 µM–30 µM) inhibits SCF- or IL-3-stimulated BMMC responses, which are not observed in PI3Kδ mutant (p110δ^D910A) cells. In anti-CD3-stimulated mice CD62L⁺ (naive) and CD62L⁻ (effector/memory) CD4⁺ T cells, IC87114 inhibits proliferation and interferon-gamma (IFN-γ) production. The IC50 values of IC87114 are: (1) 1.2 µM and 40 nM, for CD62L⁺ and CD62L⁻ cell proliferation, respectively; (2) 120 nM and 1 nM, for IFN-γ production of CD62L⁺ and CD62L⁻ cells, respectively. Similar effects by IC87114 are also observed in human T cells. A recent study reveals that in chromaffin cells, IC87114 enhances the transient increase of PtdIns(4,5)P2, which results in a potentiation of exocytosis.
in vivo	In mice, IC87114 (15 mg/kg–60 mg/kg) inhibits the allergic response in the back skin and ear. In mice induced with anti-CD3 or ConA, IC87114 (30 mg/kg) reduces hypersensitivity responses and decreases plasma levels of cytokines, such as IL-2, IL-4, IL-17, IFN-γ, and tumor necrosis factor-α (TNF-α).

プロトコル(参考用のみ)

キナーゼアッセイ	PI3K kinase assay
キナーゼアッセイ	Phosphatidylinositol-(4,5)-bisphosphate (PIP2) containing phospholipid liposomes are prepared. Briefly, bovine PIP2 and phosphatidylserine (1:2 molar ratio) are vacuum-dried and resuspended at 1 mM PIP2 in 20 mM HEPES-KOH, pH 7.4, 50 mM NaCl, and 5 mM EDTA. The lipid suspension is subjected to a brief sonication, followed by 5 freeze-thaw cycles and then 20 extrusion cycles to produce the liposomes. The assay is conducted in 60 μL reaction volumes in 20 mM HEPES, pH 7.4, buffer containing 1 nM PI3K, 1 µM PIP2, 200 µM ATP, 1 µCi [γ-³²P]ATP, 5 mM MgCl₂, plus 50 µg/mL horse IgG as carrier protein. The reaction is incubated for 10 min at room temperature, quenched in 140 of 1 M K₂PO₄, 30 mM EDTA, pH 8.0, captured onto a 96-well polyvinylidene difluoride filter plate, and washed five times with 1 M K₂PO₄. The filter is allowed to dry completely, and the bound radioactivity is quantitated. IC87114 dilutions are assayed in a final concentration of 1% (w/w) DMSO.
細胞アッセイ	細胞株	Human bone marrow mononuclear cells (BMMCs) and CD34⁺ cells
	濃度	0–100 μM
	反応時間	48 hours
	実験の流れ	For AML cell proliferation assay, BMMCs are isolated and cultured in α-medium with 5% fetal calf serum (FCS) with or without FLT-3 ligand (10 ng/mL) for 48 hours and with or without IC87114. [³H]-thymidine (1 μCi [37 kBq]) is added for a final 6 hours and the amount of radioactivity incorporated is determined by trichloracetic acid precipitation. CD34⁺ cells from cord blood are cultured in stem cell factor (SCF; 20 ng/mL), FLT-3 ligand (10 ng/mL), and Tpo (20 nM) for 48 hours with or without 10 μM IC87114 and pulsed for 12 hours with [³H]-thymidine.
動物実験	動物モデル	Wild-type or PI3Kδ mutant (p110δ^D910A) mice (C57BL/6 or BALB/c)
	投薬量	15 mg/kg–60 mg/kg
	投与方法	Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/12594293/
https://pubmed.ncbi.nlm.nih.gov/15840695/
https://pubmed.ncbi.nlm.nih.gov/15496927/

https://pubmed.ncbi.nlm.nih.gov/20081091/
https://pubmed.ncbi.nlm.nih.gov/21971506/

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カスタマーフィードバック

: Data from [J Mass Spectrom, 2012, 47(12), 1612-1619 ]

: Data from [J Mass Spectrom, 2012, 47(12), 1612-1619 ]

: , 2011, Dr. Zhang of Tianjin Medical University

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：

Downregulation of PIK3IP1/TrIP on T cells is controlled by TCR signal strength, PKC, and metalloprotease-mediated cleavage [ J Biol Chem, 2024, 300(12):107930]	PubMed: 39454954
DOCK2 and phosphoinositide-3 kinase δ mediate two complementary signaling pathways for CXCR5-dependent B cell migration [ Front Immunol, 2022, 13:982383]	PubMed: 36341455
MiR-92a/KLF4/p110δ regulates titanium particles-induced macrophages inflammation and osteolysis [ Cell Death Discov, 2022, 8(1):197]	PubMed: 35418181
Upregulated Apelin Signaling in Pancreatic Cancer Activates Oncogenic Signaling Pathways to Promote Tumor Development [ Int J Mol Sci, 2022, 23-1810600]	PubMed: 36142542
Lactobacillus rhamnosus HN001 Ameliorates BEZ235-Induced Intestinal Dysbiosis and Prolongs Cardiac Transplant Survival [ Microbiol Spectr, 2022, e0079422]	PubMed: 35862958
Impaired airway epithelial barrier integrity was mediated by PI3Kδ in a mouse model of lipopolysaccharide-induced acute lung injury [ Int Immunopharmacol, 2021, 95:107570]	PubMed: 33773208
Role of endocytosis and trans-endocytosis in ICOS costimulator-induced downmodulation of the ICOS Ligand [ J Leukoc Biol, 2021, 10.1002/JLB.2A0220-127R]	PubMed: 33527556
Distinct roles of PI3Kδ and PI3Kγ in a toluene diisocyanate-induced murine asthma model [ Toxicology, 2021, 454:152747]	PubMed: 33711354
Topical Application of the PI3Kβ-Selective Small Molecule Inhibitor TGX-221 Is an Effective Treatment Option for Experimental Epidermolysis Bullosa Acquisita [ Front Med (Lausanne), 2021, 8:713312]	PubMed: 34557502
Transient-Inhibition-of-PI3Kδ-Enhances-the-Therapeutic-Effect-of-Intravenous-Delivery-of-Oncolytic-Vaccinia-Virus. [ Mol-Ther, 2020, 6;28-5-:1263-1275]	PubMed: 32145202

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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