MP-470 TK Inhibitor
Activating or gain-of-function mutations in the c-Kit proto-oncogene have been identified in a variety of tumors including gastrointestinal stromal tumors (GIST), a very difficult tumor type to treat. MP-470 was developed to specifically bind to mutant forms of the c-Kit receptor which are insensitive to current therapies. While a potent inhibitor of wild-type c-Kit, MP-470 displays even greater effectiveness against clinically relevant mutants, including V560G, D816V, N822K and K642E, due to its unique binding mode. MP-470 is completing late-stage IND-enabling studies, for entry into the clinic in 2007.
Poster Presentations
Poster A173 AACR-NCI-EORTC 2007 MP470 Suppresses Repair of Double Strand Breaks Following Treatment with DNA-damaging Agents
Poster 1540 AACR 2007 Annual Meeting MP470.HCL, a Potent Suppressor of Rad51, Improves Bioavailability and Tolerability
Poster 4028 AACR 2007 Annual Meeting MP470, a potent suppressor of Rad51, improves response to platinum-based anticancer agents
Poster 5421 AACR 2007 Annual Meeting 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
Poster 532 EORTC-NCI-AACR 2006 c-MET Inhibition Radiosensitizes Melanoma by Inhibiting Double Strand DNA Repair
Poster 671 AACR 2008 Annual Meeting MP-470, a multi-targeted TK inhibitor in prostate and breast cancer
Poster 4083 AACR 2008 Annual Meeting MP-470, a potent oral Rad51 suppressor is safe and tolerable in first-in-human study
Poster 4891 AACR 2008 Annual Meeting Activity of the multi-targeted receptor tyrosine kinase inhibitor MP-470 against synovial sarcoma cells
MP-529 Aurora A Inhibitor
Aurora kinases are a family of oncogenic serine/threonine kinases that localize to the mitotic apparatus (centrosome, poles of the bipolar spindle, or midbody) and regulate completion of centrosome separation, bipolar spindle assembly and chromosome segregation. MP-529 is a novel inhibitor of Aurora kinases which exhibits potent activity against pancreatic tumors bearing this target, while remaining bioavailable and showing low toxicity in animal models. MP-529 is undergoing IND-enabling studies for entry into the clinic in 2007.
Poster Presentations
Poster 3261 AACR 2007 Annual Meeting Discovery and development of MP529, a new effective and selective inhibitor of Aurora A kinase
Poster 341 EORTC-NCI-AACR 2006 The discovery of MP529, a potent and selective Aurora-A kinase inhibitor, using CLIMBTM
Poster 5729 AACR 2008 Annual Meeting Pharmacokinetics of MP-529, a selective Aurora A kinase inhibitor, in a novel subcutaneous delivery system
S-110 DNMT1 Inhibitor
Silencing of unnecessary genes is commonly carried out by DNA methylation through the action of DNA Methyltransferase enzymes. However, this machinery can be usurped during the process of tumorigenesis, resulting in the inactivation of tumor suppressor genes and ultimately cancer. SuperGen is employing its proprietary CLIMB process to develop novel inhibitors of DNA Methyltransferase 1 to reverse this process in a clinical setting.
Poster Presentations
Poster B140 AACR-NCI-EORTC 2007 The Decitabine-derived Demethylating Dinucleotide S110 Shows Improved Activity Due to Increased Drug Delivery and Stability
Poster 2229 AACR 2007 Annual Meeting Zebrafish as model mechanistic screen for small molecular inhibitors of DNMT1
Poster 2613 AACR 2008 Annual Meeting The dinucleotide prodrug of decitabine demonstrated increased in vivo efficacy due to enhanced drug delivery and stabiliy
SGI-1776 Pim Kinase Inhibitor
Pim-1 is believed to play a part in tumorigenesis of a number of malignancies, including Burkitt’s Lymphoma, prostate cancer, oral cancer, and diffuse large cell lymphomas, among others. It is believed to be involved, often with the c-Myc oncoprotein, in either the initiation or progression of malignant transformation. The downstream pathways activated by Pim-1 mediate progression through the G1/S and G2/M checkpoints, and inhibition of apoptosis. Using the CLIMB process, SuperGen is hard at work on the design, synthesis and testing of a novel class of kinase inhibitor, targeting Pim-1 kinase for the treatment of various tumor types, using a combined computational and medium-throughput biological approach.
Poster Presentations
Poster 845 ASH 2007 Annual Meeting Targeting Pim Kinases in Hematological Malignancies
Poster B140 AACR-NCI-EORTC 2007 A Small Molecule Inhibitor of Pim-1 Kinase with Activity in Both Hematological and Solid Tumor Malignancies
Poster 414 EORTC-NCI-AACR 2006 Discovery and characterization of a small molecule inhibitor for Pim-1 kinase
Poster/Presentation 4974 AACR 2008 Annual Meeting A potent small molecule PIM kinase inhibitor with activity in cell lines from hematological and solid malignancies
JAK2 Kinase Inhibitor
Poster Presentations
Poster 779 ASH 2007 Annual Meeting Targeting the JAK2 Kinase in Hematological Malignancies
Poster 907 AACR-NCI-EORTC 2007 Effect of Small Molecule Inhibitors of JAK2 Kinase on Modulating Signaling Cascades Downstream of Cytokine Receptors
Poster 2387 AACR 2007 Annual Meeting Discovery and characterization of small molecule inhibitors for Jak2
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SuperGen, Inc. 2007
