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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.
| 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 |
| Molecular Weight | 417.41 |
| Formula | C19H21F2N7O2 |
| CAS Number | 475110-96-4 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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