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.
Poster Presentations
Abstract 532 EORTC-NCI-AACR 2006 c-MET Inhibition Radiosensitizes Melanoma by Inhibiting Double Strand DNA Repair
Abstract 1540 AACR 2007 Annual Meeting MP470.HCL, a Potent Suppressor of Rad51, Improves Bioavailability and Tolerability
Abstract 4028 AACR 2007 Annual Meeting MP470, a potent suppressor of Rad51, improves response to platinum-based anticancer agents
Abstract 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
Abstract 1026 AACR-NCI-EORTC 2007 MP470 Suppresses Repair of Double Strand Breaks Following Treatment with DNA-damaging Agents
Abstract 671 AACR 2008 Annual Meeting Inhibition of Erlotinib Resistance on HER family Tyrosine Kinases by Combination with MP-470, a multi-targeted TK inhibitor in Prostate &Breast Cancer
Abstract 4083 AACR 2008 Annual Meeting MP-470, a Potent Oral Rad51 Suppressor is Safe and Tolerable in First-in-human Study
Abstract 4891 AACR 2008 Annual Meeting Activity of the Multi-targeted Receptor Tyrosine Kinase Inhibitor MP-470 Against Synovial Sarcoma Cells
Abstract 393 ESMO 2008 A Phase-1 Study of MP-470, a Novel Orally Bioavilable Small Molecule with Rad51 Suppression Activity
Abstract 403 EORTC-NCI-AACR 2008 Clinical Responses in Highly Refractory Solid Tumor Patients with Oral MP-470, a Multi-Targeted Tyrosine Kinase Inhibitor, in Combination with Standard of Care Chemotherapy Regimens: Preliminary Report from a Multi-Institutional Phase-1b Clinical Trial
Abstract 426 EORTC-NCI-AACR 2008 Effects of Food on the Single-Dose Pharmacokinetics of Oral MP-470 Capsules
Abstract 480 EORTC-NCI-AACR 2008 MP-470, A Novel Multi-Targeted Tyrosine Kinase Inhibitor Targeting Rad 51 is Not Toxic to Human Primary Marrow Stem Cells at Clinically Relevant Concentrations
Abstract 48 7th International Symposium on Targeted Anticancer Therapies Meeting Effects of MP-470 on pharmacokinetics of carboplatin, paclitaxel and etoposide
Abstract 3729 AACR 2009 Annual Meeting MP-470, a Rad51 Suppressor and Multiple TK Inhibitor, Retards Growth of Primary Human Glioblastoma Multiforma (GBM) Cells and Synergizes Effect of Temozolomide
Abstract 3728 AACR 2009 Annual Meeting MP-470, a Small Molecule Tyrosine Kinase Inhibitor, Induces Apoptosis in Multiple Myeloma Cells
Abstract 337 2009 EMCTO Conference A Phase 1b Dose Escalation Study of MP-470 Administered Concurrently with Standard of Care Chemotherapy in Patients with NSCLC and SCLC
Journal Article BMC Cancer 2009, 9:142 MP-470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer
Abstract # e13511 ASCO 2009 Annual Meeting, e-publication A phase Ib dose-escalation study of orally administered MP-470, a multi-kinase inhibitor and supressor of Rad51, in combination with carboplatin doublet containing regimens shows activity in highly refractory solid tumor patients.
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.
Poster Presentations
Abstract 341 EORTC-NCI-AACR 2006 The discovery of MP529, a potent and selective Aurora-A kinase inhibitor, using CLIMBTM
Abstract 3261 AACR 2007 Annual Meeting Discovery and development of MP529, a new effective and selective inhibitor of Aurora A kinase
Abstract 5729 AACR 2008 Annual Meeting Pharmacokinetics of MP-529, a selective Aurora A kinase inhibitor, in a novel subcutaneous delivery system
Abstract 3725 AACR 2009 Annual Meeting Identifying Sensitizers of Aurora Kinase Inhibitors by High-throughput siRNA Screening
SGI-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
Abstract 2229 AACR 2007 Annual Meeting Zebrafish as model mechanistic screen for small molecular inhibitors of DNMT1
Abstract 1038 AACR-NCI-EORTC 2007 The Decitabine-derived Demethylating Dinucleotide S110 Shows Improved Activity Due to Increased Drug Delivery and Stability
Abstract 2613 AACR 2008 Annual Meeting The dinucleotide prodrug of decitabine demonstrated increased in vivo efficacy due to enhanced drug delivery and stabiliy
Abstract 3355 ASH 2008 Annual Meeting 3355 Anti-AML Activity of Combined Epigenetic Therapy with Novel DNMT1 Inhibitors SGI-110 and SGI-1036 and Histone Deacetylase Inhibitor Panobinostat
SGI-1776 Pim Kinase Inhibitor
Pim-1 is believed to play a part in tumorigenesis of a number of malignancies, including acute myelogenous leukemia, 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
Abstract 414 EORTC-NCI-AACR 2006 Discovery and characterization of a small molecule inhibitor for Pim-1 kinase
Abstract 985 AACR-NCI-EORTC 2007 A Small Molecule Inhibitor of Pim-1 Kinase with Activity in Both Hematological and Solid Tumor Malignancies
Abstract 2655 ASH 2007 Annual Meeting Targeting Pim Kinases in Hematological Malignancies
Abstract/Oral Presentation 4974 AACR 2008 Annual Meeting A potent small molecule PIM kinase inhibitor with activity in cell lines from hematological and solid malignancies
Abstract 0278 13th Congress of the EHA 2008 A Potent Small Molecule Pim Kinase Inhibitor with In Vivo Oral Availability and Activity in Cell Lines From Hematological Malignancies
Abstract 332 EORTC-NCI-AACR 2008 In Vivo Activity of SGI-1776, an Orally Active Pim Kinase Inhibitor
Abstract 1922 ASH 2008 Annual Meeting Inhibiting PIM-1 Is Effective in Vitro and in Vivo against ALL: A Novel Mechanistic and Potentially Clinically Relevant Druggable Target
Poster 106 2009 Targeted Cancer Therapies Meeting Evaluation of the Anticancer Activity of SGI-1776, a Novel PIM Kinase Inhibitor, In Solid tumor and Hematologic Cancer Cells
Abstract/Oral Presentation 2013 AACR 2009 Annual Meeting Discovery of SGI-1776, a Potent and Selective PIM-1 Kinase Inhibitor
Abstract 3743 AACR 2009 Annual Meeting SGI-1776: A Novel Pim Kinase Inhibitor with Potent Preclinical Activity Against Acute Myeloid Leukemia
Abstract 1090 EHA 2009 Congress ExVivo Activity of SGI-1776, a Potent Small Molecule PIM KInase Inhibitor, in Primary Human Leukemia and Lymphoma Cells
SGI-1252 JAK2 Kinase Inhibitor
Poster Presentations
Abstract 2387 AACR 2007 Annual Meeting Discovery and characterization of small molecule inhibitors for Jak2
Abstract 907 AACR-NCI-EORTC 2007 Effect of Small Molecule Inhibitors of JAK2 Kinase on Modulating Signaling Cascades Downstream of Cytokine Receptors
Abstract 3560 ASH 2007 Annual Meeting Targeting the JAK2 Kinase in Hematological Malignancies
Abstract 571 EORTC-NCI-AACR 2008 Modulation of JAK2 Signalint Pathways In Vitro and In VIvo by SGI-1252, A Potent Small Molecule JAK2 Inhibitor
Abstract 2629 ASH 2008 Annual Meeting Preclinical Characterization of the JAK-2 Inhibitor, SGI-1252
Poster 204 2009 Targeted Cancer Therapies Meeting Preliinical characterization of SGI-1252, a potent, selective, adn oral inhibitor of janus kinases: modulation of inflamatory and immuno-modulatory pathways
ETK Inhibitor
Poster Presentations
Abstract 3745 AACR 2009 Annual Meeting Targeting ETK/BMX Kinase with Small Molecule Inhibitors
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SuperGen, Inc. 2007
