Eganelisib (Synonyms: IPI-549)

目录号: HY-100716 纯度: 99.68%: Data Sheet SDS COA 产品使用指南
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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。

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Eganelisib Chemical Structure

CAS No. : 1693758-51-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥814	In-stock
1 mg	￥318	In-stock
5 mg	￥700	In-stock
10 mg	￥1100	In-stock
25 mg	￥2200	In-stock
50 mg	￥3300	In-stock
100 mg	￥4950	In-stock
500 mg	现货	询价
1 g		询价
5 g		询价

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Customer Review

MCE 顾客使用本产品发表的 18 篇科研文献

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases^[1].

IC₅₀ & Target^[1]

PI3Kγ

16 nM (IC₅₀)

PI3Kα

3.2 μM (IC₅₀)

PI3Kβ

3.5 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Raji	IC₅₀	180 nM Compound: 26	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 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	[PMID: 27660692]
RAW264.7	IC₅₀	1.2 nM Compound: 26	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 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	[PMID: 27660692]
Sf9	IC₅₀	> 8400 nM Compound: 26	Inhibition of human recombinant full length N-terminal GST-tagged PI3K p110delta/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 Inhibition of human recombinant full length N-terminal GST-tagged PI3K p110delta/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	[PMID: 27660692]
Sf9	IC₅₀	16 nM Compound: 26	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 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	[PMID: 27660692]
Sf9	IC₅₀	3200 nM Compound: 26	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 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	[PMID: 27660692]
Sf9	IC₅₀	3500 nM Compound: 26	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 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	[PMID: 27660692]
SK-OV-3	IC₅₀	250 nM Compound: 26	Inhibition of PI3Kalpha in human SKOV-3 cells assessed as reduction in AKT phosphorylation at S473 after 30 mins by ELISA Inhibition of PI3Kalpha in human SKOV-3 cells assessed as reduction in AKT phosphorylation at S473 after 30 mins by ELISA	[PMID: 27660692]

体外研究
(In Vitro)

Eganelisib (IPI549) 对 PI3Kγ 的抑制 IC₅₀ 为 16 nM，且对其他脂质和蛋白激酶的选择性超过 100 倍 (PI3Kα IC₅₀=3.2 μM，PI3Kβ IC₅₀=3.5 μM，PI3Kδ IC₅₀>8.4 μM)。研究评估了 Eganelisib 对所有 I 类 PI3K 亚型的抑制活性。通过测定结合速率常数和平衡荧光滴定法，分别确定了 Eganelisib 与 PI3K-γ 的结合亲和力，以及对 PI3K-α、β 和 δ 的亲和力。Eganelisib 与 PI3Kγ 的结合非常紧密，K_d 值为 290 pM，而对其他 I 类 PI3K 亚型的亲和力弱 58 倍以上 (PI3Kα K_d=17 nM，PI3Kβ K_d=82 nM，PI3Kδ K_d=23 nM)。在依赖于 PI3K-α、-β、-γ 和 -δ 的细胞磷酸化 AKT 检测中，Eganelisib 表现出优异的 PI3K-γ 抑制效力 (IC₅₀=1.2 nM) 和对其他 I 类 PI3K 亚型的选择性 (>146 倍)。通过 ELISA 法检测 pAKT S473 的抑制情况，分别在 SKOV-3、786-O、RAW 264.7 和 RAJI 细胞中测定了依格那利塞对 I 类 PI3Kα (250 nM)、PI3Kβ (240 nM)、PI3Kγ (1.2 nM) 和 PI3Kδ (180 nM) 的细胞 IC₅₀ 值。此外，Eganelisib 呈剂量依赖性抑制 PI3Kγ 依赖的骨髓源性巨噬细胞 (BMDM) 迁移。在 10 μM 浓度下，Eganelisib 对 80 种 GPCR、离子通道和转运蛋白具有选择性^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Eganelisib (IPI549) 展现出良好的药代动力学特性，并能强力抑制 PI3K-γ 介导的中性粒细胞迁移。在动物体内实验 (小鼠、大鼠、犬和猴) 中，Eganelisib 具有优异的口服生物利用度、低清除率，且能广泛分布于组织中，平均分布容积为 1.2 L/kg。总体而言，Eganelisib 具备良好的药代动力学特征，可在体内实现 PI3K-γ 的强效选择性抑制。IPI-549 在小鼠、大鼠、犬和猴体内的 t_1/2 分别为 3.2、4.4、6.7 和 4.3 小时。在该模型中，所有测试剂量下口服给药的 Eganelisib 均能呈剂量依赖性显著减少中性粒细胞迁移^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

528.56

Formula

C₃₀H₂₄N₈O₂

CAS 号

1693758-51-8

性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (47.30 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8919 mL	9.4597 mL	18.9193 mL
5 mM	0.3784 mL	1.8919 mL	3.7839 mL
10 mM	0.1892 mL	0.9460 mL	1.8919 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.73 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.73 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.68%

选择批次：

Data Sheet (656 KB) SDS (393 KB)

COA (291 KB) HNMR (298 KB) LCMS (94 KB) 元素分析报告 (214 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Evans CA, et al. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. [Content Brief]

[2]. De Henau O, et al. Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells. Nature. 2016 Nov 17;539(7629):443-447. [Content Brief]

Animal Administration ^[2]	C57BL/6J and Balb/c mice (6 to 8 weeks old) are used in this study. On day 0 of the experiments, tumor cells are injected intradermally (i.d.) in the right flank. Eganelisib is administered by oral gavage once a day at 15 mg/kg. Treatment is initiated on day 7 ending on day 21 post tumor implant. Control groups receive vehicle (5% NMP, 95% PEG). Tumors are measured every second or third day with a caliper, and the volume (length×width×height) is calculated. Animals are euthanized for signs of distress or when the total tumor volume reaches 2500 mm³. Finally, Tumors are isolated, and frozen until needed^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Evans CA, et al. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. [Content Brief] [2]. De Henau O, et al. Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells. Nature. 2016 Nov 17;539(7629):443-447. [Content Brief]

Animal Administration
^[2]

C57BL/6J and Balb/c mice (6 to 8 weeks old) are used in this study. On day 0 of the experiments, tumor cells are injected intradermally (i.d.) in the right flank. Eganelisib is administered by oral gavage once a day at 15 mg/kg. Treatment is initiated on day 7 ending on day 21 post tumor implant. Control groups receive vehicle (5% NMP, 95% PEG). Tumors are measured every second or third day with a caliper, and the volume (length×width×height) is calculated. Animals are euthanized for signs of distress or when the total tumor volume reaches 2500 mm³. Finally, Tumors are isolated, and frozen until needed^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Evans CA, et al. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. [Content Brief]

[2]. De Henau O, et al. Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells. Nature. 2016 Nov 17;539(7629):443-447. [Content Brief]

Eganelisib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8919 mL	9.4597 mL	18.9193 mL	47.2983 mL
	5 mM	0.3784 mL	1.8919 mL	3.7839 mL	9.4597 mL
	10 mM	0.1892 mL	0.9460 mL	1.8919 mL	4.7298 mL
	15 mM	0.1261 mL	0.6306 mL	1.2613 mL	3.1532 mL
	20 mM	0.0946 mL	0.4730 mL	0.9460 mL	2.3649 mL
	25 mM	0.0757 mL	0.3784 mL	0.7568 mL	1.8919 mL
	30 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5766 mL
	40 mM	0.0473 mL	0.2365 mL	0.4730 mL	1.1825 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Eganelisib1693758-51-8IPI-549IPI549IPI 549PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Eganelisib (Synonyms: IPI-549)

Customer Review

MCE 顾客使用本产品发表的 18 篇科研文献