ZSTK474

Name: ZSTK474
Brand: MedChemExpress
SKU: HY-50847
Rating: 5.0 (18 reviews)

Cat. No.: HY-50847 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

ZSTK474 Chemical Structure

CAS No. : 475110-96-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 46	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 46	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 125	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 185	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 18 publication(s) in Google Scholar

17 Publications Citing Use of MCE ZSTK474

: ZSTK474 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122. [Abstract]; MHCC97H cells are treated with either LY294002 (2.5, 5,10, 20, 40 μM) or ZSTK474 (0.5, 1, 2.5, 5, 10 μM) for 24 h. DMSO is used as the control. Cell lysates are subjected to western blot analysis with the indicated antibodies.

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View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

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]

In Vitro

Lineweaver-Burk plot analysis revealed that ZSTK474 inhibits all four PI3K isoforms in an ATP-competitive manner. The K_i values determined for the four PI3K isoforms showed that ZSTK474 inhibited the PI3Kδ isoform most effectively with a K_i of 1.8 nM, whereas the other isoforms are inhibited with 4-10-fold higher K_i values. Therefore, ZSTK474 should be regarded as a pan-PI3K inhibitor. We also determined the IC₅₀ values for inhibiting the four PI3K isoforms with ZSTK474 and LY294002. The IC₅₀ values of ZSTK474 (16, 44, 4.6 and 49 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively) are shown to be consistent with the K_i values (6.7, 10.4, 1.8 and 11.7 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively), which further supported the idea that ZSTK474 inhibits PI3Kδ most potently. Even at a concentration of 100 μM, ZSTK474 inhibits mTOR activity rather weakly^[1].

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

In Vivo

In mice subjected to MCAO, treatment with ZSTK474 is tested at dosages of 50, 100, 200, and 300 mg/kg. Since the 200 mg/kg dose produces significant improvement and no obvious toxic effects (P<0.01), mice are treated with ZSTK474 at a dose of 200 mg/kg/day daily for three post-MCAO days during the remaining experiments of this study. Neurological function is examined in mice suffered from MCAO followed by 24, 48, and 72 h of reperfusion. In the ZSTK474 group, neurological function scores are significantly better than the control group except the corner test^[2].

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

Clinical Trial

Molecular Weight

417.41

Formula

C₁₉H₂₁F₂N₇O₂

CAS No.

475110-96-4

Appearance

Solid

Color

White to off-white

SMILES

FC(C1=NC2=C(N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)C=CC=C2)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (79.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (287 KB) SDS (252 KB)

COA (259 KB) HNMR (393 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

ZSTK474 Related Classifications

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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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ZSTK474

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ZSTK474 Related Antibodies

17 Publications Citing Use of MCE ZSTK474

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