ZSTK474 Chemical Structure
BEZ235 (NVP-BEZ235)is a dual ATP-competitive phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM,respectively.
Perifosine is an Akt inhibitor. the antiproliferative properties of perifosine with an IC50 of 0.6–8.9 µM.
PI-103 is a potent, cell-permeable, ATP-competitive PI3K family member inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.
Inhibitor of Class I PI3 Kinase,p110a IC50=0.003uM,U87MG IC50=0.95μM.
LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.
XL147 is a selective inhibitor of Class I PI3K isoforms.
TGX-221 is a low-nanomolar range PI3Kβ inhibitor (IC50=10nM), shows about 1000-fold higher selectivity over PI3Kα, and is cell permeable. Order TGX-221 from supplier Selleck for research use only.
PIK-90 is a PI3K inhibitor,IC50=11, 350, 18, and 58 for p110 α, β, γ and δ isoforms.
PIK-75 Hydrochloride is a hydrochloride salt form of PIK-75, which is a preferential p110α/γ forms of PI3K inhibitor with IC50 of 6, 1300, 76, 510 nM for p110α, p110β, p110γ, p110δ, respectively.
YM201636 is a novel PIKfyve-specific inhibitor with an IC50 of 54 nM for the net insulin response.
ZSTK474 is an inhibitor of PI3K γ (IC50 at 6 nM). This agent inhibits PI3K α and PI3K β with IC50 of 17 and 53 nM, respectively. ZSTK474 was identified from a chemical library of about 1500 triazine derivatives, and selected for their ability to block tumor cell growth. In preclinical studies ZSTK474 was orally administered to mice and displayed a strong anti-tumoral activity in xenograft models. Toxicity was reported to be moderate. [1]
| Molecular Weight (WM): | 417.41 |
|---|---|
| Formula: | C19H21F2N7O2 |
| CAS No.: | 475110-96-4 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO ≥21mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
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We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
Data independently produced by Saraswati Sukumar of Johns Hopkins University School of Medicine---ZSTK474 purchased from Selleck ZSTK474 purchased from Selleck

Western blot analysis of Akt and p-Akt. 0-20μM ZSTK474 was added. |
Western blot analysis of Akt and p-Akt. 0-20μM ZSTK474 was added.
Data independently produced by Dr. Zhang of Tianjin Medical University ZSTK474 purchased from Selleck
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