| Chemical Properties | Back Directory | [Boiling point ]
608.4±55.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≤0.25mg/ml in ethanol;5mg/ml in DMSO;10mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
4.24±0.10(Predicted) | [color ]
Light yellow to orange |
| Hazard Information | Back Directory | [Description]
The tumor suppressor gene, p53, is often mutated or suppressed in human cancers. Oncogenic K-Ras has been shown to inhibit p53 function by inducing Snail to bind and eliminate p53 through exocytosis. GN25 is a 2-thio-dimethoxy naphthoquinone analog that blocks Snail binding to p53 and induces p53 expression in cancer cells in a K-Ras dependent manner. At 10 μM, GN25 significantly reduces cell proliferation in K-Ras mutated A549 and HCT116 cell lines but not in wild type MKN-45 cells. In a xenograft mouse model, 10 mg/kg GN25 yields antitumoral effects by notably reducing tumor size and progression. | [Uses]
GN25 is a specific p53-Snail binding inhibitor with antitumor effects[1]. | [in vivo]
GN25 (10 and 20 mg/kg; i.p. once a week for 10 weeks) blocks the tumor progression and induces tumor regression in mice[1]. | Animal Model: | Athymic mice with A549 xenografts[1] | | Dosage: | 10 and 20 mg/kg | | Administration: | Intraperitoneal injection; once a week for 10 weeks | | Result: | Obviously regressed tumors in mice. Showed no significant toxicity in liver, pancreas and kidney.
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| [References]
[1]. lee sh, shen gn, jung ys, et al. antitumor effect of novel small chemical inhibitors of snail-p53 binding in k-ras-mutated cancer cells. oncogene. 2010 aug 12;29(32):4576-87. |
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