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ZSTK474

Cat. No. M1878
ZSTK474 Structure
Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 220 In stock
100mg USD 360 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

ZSTK474 is a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, which strongly inhibits cancer cell proliferation. Phosphoinositide 3-kinase (PI3K) is a potential target in cancer therapy. Inhibition of PI3K is believed to induce apoptosis. ZSTK474 effectively inhibited the growth of human cancer xenografts in vivo. ZSTK474 treatment suppressed the expression of nuclear cyclin D1 and Ki67 and also the expression of phospho-Akt, both of which are hallmarks of proliferation. We demonstrate that ZSTK474 induces G1arrest along with tumour suppression. Moreover, ZSTK474 suppresses the tumour growth without inducing apoptosis. Interestingly, long-term (3-month) administration of ZSTK474 maintained such increase in G1 cells and tumour suppression. ZSTK474 exerts its in vivo antitumour efficacy via G1 arrest but not via apoptosis as long as it is administered.

Protocol
Cell Experiment
Cell lines panel of 39 human cancer cell lines
Preparation method Analysis of Cell Proliferation Inhibition
The inhibition of cell proliferation was assessed by measuring changes in total cellular protein in a culture of each cell line in the JFCR panel of cell lines after 48 hours of drug treatment by use of a sulforhodamine B assay. The 50% growth inhibition (GI 50 ) value of the drug was calculated as described previously. The graphic representation of a drug’s mean differential growth inhibition for the cell line panel was based on a calcula-tion that used a set of GI 50 values, as described previously. To analyze the correlation between the mean graphs of drug A and drug B, the COMPARE computer algorithm was developed as previously described by Paull et al. The Pearson correla-tion coeffi cient between the mean graphs of drug A and drug B was calculated (n = 39).
Concentrations 0~10μM
Incubation time 48 h
Animal Experiment
Animal models Human A549 lung cancer cells, PC-3 prostate cancer cells, and WiDr colon cancer cells tumor xenografts
Formulation 5% hydroxypropylcellulose in water
Dosages 100, 200, or 400 mg/kg daily from days 0 to 13
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 417.41
Formula C19H21F2N7O2
CAS Number 475110-96-4
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor.
Yaguchi S, et al. J Natl Cancer Inst. 2006 Apr 19;98(8):545-56. PMID: 16622124.

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  Catalog
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Keywords: ZSTK474 supplier, PI3K, inhibitors

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