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Data Show SuperGen's Multi-Targeted Tyrosine Kinase Inhibitor,Suppresses Critical Double-Stranded DNA Repair Protein, Rad51

and exocrine pancreas, all of which are easily visualized. This screen allows quick validation of DNMT1 inhibition in vivo, as well as important data on the toxicity of compounds tested.

Abstract No. 3261

Discovery and development of MP529, a new effective and selective inhibitor of Aurora A kinase

MP529 series compounds, such as SGI-498, SGI-503, SGI-1097 and SGI-1215, demonstrate potent nanomolar inhibitory activity against the Aurora-A enzyme in biochemical enzyme-based assays, while exhibiting little to no activity versus the Aurora B kinase. SuperGen developed this series of lead compounds for use in anticancer therapy using rational-based drug design. Extensive in silico screening reduced the number of compounds submitted to physical assays to fewer than 100, saving significant time and resources over standard drug discovery practices. The series of compounds was evaluated in in vivo xenograft models and showed efficacy while maintaining desirable pharmacokinetic properties.

Abstract No. 5421

Dual inhibition of receptor tyrosine kinases of PDGFR and EGFR abolishes prostate cancer cell growth in culture and in a mouse xenograft model by complete dephosphorylation of PKB/Akt

MP470, SuperGen's multi-targeted tyrosine kinase inhibitor, in combination with Tarceva was more effective than either treatment alone in the inhibition of cell proliferation and phosphorylation of Akt in EGF and PDGF pathways. Moreover, in combination with Tarceva, MP470 inhibited Akt phosphorylation in LNCaP prostate cells. Finally, the MP470/Tarceva treatment was shown to abolish prostate tumor growth in an LNCaP xenograft mouse model

Mini-symposium Abstract No. 4142

Novel DNA hypomethylating agents: non-nucleoside compounds that do not incorporate into DNA selectively induce degradation of DNA methyltransferase I (DNMT1) in human cancer cells by the proteasomal pathway and re-express silenced tumor suppressor genes

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