ZSTK474

目录号: HY-50847 纯度: 99.71%: Data Sheet SDS COA 产品使用指南
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ZSTK474 是一种 ATP 竞争性的泛 I 类 PI3K 抑制剂，抑制 PI3Kα，PI3Kβ，PI3Kδ 和 PI3Kγ，IC₅₀ 分别为 16 nM，44 nM，4.6 nM 和 49 nM。

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ZSTK474 Chemical Structure

CAS No. : 475110-96-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥338	In-stock
5 mg	￥308	In-stock
10 mg	￥515	In-stock
50 mg	￥1700	In-stock
100 mg	￥3100	In-stock
200 mg	￥4863	In-stock
500 mg		询价
1 g		询价

or 大包装询价

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Customer Review

MCE 顾客使用本产品发表的 17 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

ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC₅₀s of 16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.

IC₅₀ & Target^[2]

PI3Kδ

4.6 nM (IC₅₀)

PI3Kα

16 nM (IC₅₀)

PI3Kβ

44 nM (IC₅₀)

PI3Kγ

49 nM (IC₅₀)

Autophagy

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	1.31 μM Compound: ZSTK474	Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay	[PMID: 30245395]
HCT-116	IC₅₀	1.31 μM Compound: ZSTK474	Antiproliferative activity against human HCT116 cells harboring PI3Kalpha H1047R mutant after 72 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells harboring PI3Kalpha H1047R mutant after 72 hrs by CCK8 assay	[PMID: 30071408]
HCT-116	IC₅₀	78 nM Compound: 1, ZSTK474	Inhibition of PIK3CA H1047R mutant-mediated cell signaling in human HCT116 cells expressing PTEN assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblott Inhibition of PIK3CA H1047R mutant-mediated cell signaling in human HCT116 cells expressing PTEN assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblott	[PMID: 21882832]
HCT-116	IC₅₀	97 nM Compound: 1, ZSTK474	Inhibition of PIK3CA H1047R mutant-mediated cell signaling in human HCT116 cells expressing PTEN assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblott Inhibition of PIK3CA H1047R mutant-mediated cell signaling in human HCT116 cells expressing PTEN assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblott	[PMID: 21882832]
HT-29	GI₅₀	300 nM Compound: ZSTK474	Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay	[PMID: 33284613]
LNCaP	IC₅₀	210 nM Compound: 6	Antiproliferative activity against human LNCAP cells after 3 days by MTS assay Antiproliferative activity against human LNCAP cells after 3 days by MTS assay	[PMID: 20227881]
MCF7	IC₅₀	5.27 μM Compound: ZSTK474	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells after 72 hrs by CCK-8 assay	[PMID: 30245395]
MCF7	IC₅₀	5.27 μM Compound: ZSTK474	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 30071408]
MDA-MB-468	EC₅₀	3.2 μM Compound: ZSTK474	Cytotoxicity against PTEN-deficient human MDA-MB-468 cells assessed as inhibition of cell growth after 48 hrs by Cell Titer 96 assay Cytotoxicity against PTEN-deficient human MDA-MB-468 cells assessed as inhibition of cell growth after 48 hrs by Cell Titer 96 assay	[PMID: 23795239]
Sf21	IC₅₀	0.003 μM Compound: 4a, ZSTK474	Inhibition of PI3Kdelta (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay Inhibition of PI3Kdelta (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay	[PMID: 23265896]
Sf21	IC₅₀	0.006 μM Compound: 4a, ZSTK474	Inhibition of PI3Kbeta (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay Inhibition of PI3Kbeta (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay	[PMID: 23265896]
Sf21	IC₅₀	0.006 μM Compound: 4a, ZSTK474	Inhibition of PI3Kalpha (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay Inhibition of PI3Kalpha (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay	[PMID: 23265896]
Sf21	IC₅₀	0.038 μM Compound: 4a, ZSTK474	Inhibition of PI3Kgamma (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay Inhibition of PI3Kgamma (unknown origin) expressed in SF21 cells using phosphatidylinositol as substrate after 60 mins by Kinase-Glo assay	[PMID: 23265896]
Sf21	IC₅₀	6 nM Compound: ZSTK-47	Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay	[PMID: 27387421]
U-87MG ATCC	IC₅₀	111 nM Compound: 1, ZSTK474	Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting	[PMID: 21882832]
U-87MG ATCC	IC₅₀	32 nM Compound: 1, ZSTK474	Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting	[PMID: 21882832]

体外研究
(In Vitro)

Lineweaver-Burk 图分析显示 ZSTK474 以 ATP 竞争性方式抑制所有四种 PI3K 亚型。对四种 PI3K 亚型测定的 Ki 值表明 ZSTK474 对 PI3Kδ 亚型抑制最有效，Ki 为 1.8 nM，而对其他亚型的抑制 Ki 值高出 4-10 倍。因此，ZSTK474 应被视为泛 PI3K 抑制剂。作者还测定了 ZSTK474 和 LY294002 抑制四种 PI3K 亚型的 IC₅₀ 值。 ZSTK474 对 PI3Kα、PI3Kβ、PI3Kδ 和 PI3Kγ 的 IC₅₀ 值分别为 16、44、4.6 和 49 nM）与 Ki 值分别为 6.7、10.4、1.8 和 11.7 nM，这进一步支持了 ZSTK474 对 PI3Kδ 抑制最强的观点。即使在 100 μM 浓度下，ZSTK474 对 mTOR 活性的抑制也相当弱^[1]。

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

体内研究
(In Vivo)

在遭受 MCAO 的小鼠中，以 50、100、200 和 300 mg/kg 的剂量测试 ZSTK474 的效果。由于 200 mg/kg 剂量产生显著改善且无明显毒性作用 (P<0.01)，因此在本研究的其余实验中，小鼠在 MCAO 后三天每天以 200 mg/kg/天的剂量接受 ZSTK474 治疗。在遭受 MCAO 的小鼠中检查神经功能，随后进行 24、48 和 72 小时的再灌注。在 ZSTK474 组中，除角落测试外，神经功能评分明显优于对照组^[2]。

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

Clinical Trial

分子量

417.41

Formula

C₁₉H₂₁F₂N₇O₂

CAS 号

475110-96-4

性状

固体

颜色

White to off-white

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 33.33 mg/mL (79.85 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	2.3957 mL	11.9786 mL	23.9573 mL
5 mM	0.4791 mL	2.3957 mL	4.7915 mL
10 mM	0.2396 mL	1.1979 mL	2.3957 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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：

以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

方案一

ZSTK474 is suspended in 5% hydroxypropyl cellulose^[3].

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

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.71%

选择批次：

Data Sheet (633 KB) SDS (393 KB)

COA (296 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Kong D, et al. ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms. Cancer Sci, 2007, 98(10), 1638-1642. [Content Brief]

[2]. Liu F, et al. Prolonged inhibition of class I PI3K promotes liver cancer stem cell expansion by augmenting SGK3/GSK-3β/β-catenin signalling. J Exp Clin Cancer Res. 2018 Jun 25;37(1):122. [Content Brief]

[3]. Wang P, et al. Class I PI3K inhibitor ZSTK474 mediates a shift in microglial/macrophage phenotype and inhibits inflammatory response in mice with cerebral ischemia/reperfusion injury. J Neuroinflammation. 2016 Aug 22;13(1):192. [Content Brief]

Kinase Assay ^[1]	The linear phase of each kinetic reaction is defined at the respective enzyme amount (0.05, 0.1, 0.12 and 1 µg/mL for PI3Kα, PI3β, PI3δ and PI3γ, respectively) and reaction time (20 min). PI3K activity is assayed at various concentrations of ATP (5, 10, 25, 50, 100 µM) in the presence of increasing concentrations of ZSTK474. A Lineweaver-Burk plot is developed by plotting 1/v (the inverse of v, where v is obtained by subtracting the HTRF signal of the kinase test sample from the HTRF signal of the minus-enzyme control) versus 1/[ATP] (the inverse of the ATP concentration). For the minus-enzyme control, PIP2 is incubated with ATP in the absence of kinase. To determine the K_i value (inhibition constant) of ZSTK474 for each PI3K isoform, the slope of the respective Lineweaver-Burk plot is replotted against the ZSTK474 concentration. The K_i values are calculated by analysis using GraphPad Prism 4^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] Mice are randomly assigned to receive different doses of ZSTK474 (50, 100, 200, and 300 mg/kg) to determine the optimum dose; in our experiment, the optimum dose is 200 mg/kg. Then mice are randomly assigned to one of three groups: a sham-operated group (phosphate-buffered saline, PBS); a control group (MCAO+PBS); a ZSTK474-treated group (MCAO+ZSTK474). In the ZSTK474-treated group, the mice are given the optimum dose of 200 mg/kg ZSTK474. In the sham-operated group and control group, mice are given an equivalent volume of PBS. All mice receive that same dose daily via oral gavage beginning at 6 h after the onset of focal ischemia and continuing for two more days, i.e., for a total of 3 days. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Kong D, et al. ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms. Cancer Sci, 2007, 98(10), 1638-1642. [Content Brief] [2]. Liu F, et al. Prolonged inhibition of class I PI3K promotes liver cancer stem cell expansion by augmenting SGK3/GSK-3β/β-catenin signalling. J Exp Clin Cancer Res. 2018 Jun 25;37(1):122. [Content Brief] [3]. Wang P, et al. Class I PI3K inhibitor ZSTK474 mediates a shift in microglial/macrophage phenotype and inhibits inflammatory response in mice with cerebral ischemia/reperfusion injury. J Neuroinflammation. 2016 Aug 22;13(1):192. [Content Brief]

ZSTK474 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	2.3957 mL	11.9786 mL	23.9573 mL	59.8932 mL
	5 mM	0.4791 mL	2.3957 mL	4.7915 mL	11.9786 mL
	10 mM	0.2396 mL	1.1979 mL	2.3957 mL	5.9893 mL
	15 mM	0.1597 mL	0.7986 mL	1.5972 mL	3.9929 mL
	20 mM	0.1198 mL	0.5989 mL	1.1979 mL	2.9947 mL
	25 mM	0.0958 mL	0.4791 mL	0.9583 mL	2.3957 mL
	30 mM	0.0799 mL	0.3993 mL	0.7986 mL	1.9964 mL
	40 mM	0.0599 mL	0.2995 mL	0.5989 mL	1.4973 mL
	50 mM	0.0479 mL	0.2396 mL	0.4791 mL	1.1979 mL
	60 mM	0.0399 mL	0.1996 mL	0.3993 mL	0.9982 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:

ZSTK474475110-96-4ZSTK 474ZSTK-474PI3KAutophagyPhosphoinositide 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）

ZSTK474

Customer Review

MCE 顾客使用本产品发表的 17 篇科研文献