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SF1126, Semafore's PI3 Kinase Inhibitor, Found to Block Angiogenic Signaling From Both VEGF and Bv8 in Multiple Cell Lines
Date:8/26/2008

any's focus - cancer. Semafore is a leader in the development of PI3K inhibitors and one of the first biopharmaceutical companies to focus on both PI3K and PTEN. The company has successfully discovered and is developing a portfolio of drug candidates addressing these targets.

About SF1126

There is a strong and significant biological rationale for developing PI3 kinase inhibitors to treat cancer. Phosphoinositide 3-kinase (PI3K) is the gate keeper of one of the major pathways of intracellular signal transduction that regulates cell growth, proliferation, angiogenesis, migration, differentiation, and survival. Dysregulation of the PI3K signaling pathway is believed to play an integral role in the genesis of many cancers including both solid tumors and hematologic malignancies. Cancer research and pharmaceutical drug development efforts have been aimed at discovering and developing therapeutics that inhibit PI3K with the hope of controlling cancer cell division, angiogenesis (the formation of new blood vessels for cancer

growth), proliferation and metastasis. Semafore's innovative PI3K inhibitor, SF1126, promises such hope for cancer patients.

SF1126, is a proprietary small molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class I isoforms and other key members of the PI3K superfamily, including mTOR, DNA-PK, PLK-1,CK2, ATM and PIM-1 kinases all known to be involved in the cascade of chemical signals that control cell division. Importantly, SF1126 is designed as a dual inhibitor of both angiogenesis and cell proliferation. SF1126 is engineered to target and bind to specific integrins (alpha gamma beta 3) that are expressed on the surface of new tumor vasculature and within the tumor endothelial compartment. In tumor xenograph models Semafore demonstrated enhanced drug uptake of SF1126 which was directly attributable to the alpha gamma beta 3 targeted moiety. SF1126 is water soluble, has favorable pharmacok
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SOURCE Semafore Pharmaceuticals Inc.
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Related medicine technology :

1. Semafore Pharmaceuticals Reports Positive Interim Results from a Phase I Study of SF1126, a Targeted Pan-PI3K Inhibitor, in Patients with Advanced Solid Tumors
2. Telik Announces Presentation of Preclinical Data on Dual Inhibitors of Aurora Kinases and VEGFR2
3. Telik Announces Preclinical Data Demonstrating Anti-Cancer Activity of Dual Inhibitors of Aurora Kinase and VEGFR2
4. Semafores PI3 Kinase Inhibitor SF1126 is Active Against Tumor and Tumor Cells and Synergizes with Standard Chemotherapy Agents
5. SuperGen Reports Initiation of Multi-arm Phase 1b Trial of Novel Tyrosine Kinase Inhibitor
6. EntreMed to Highlight ENMD-2076 Kinase Inhibitor at 2008 AACR Annual Meeting
7. Semafores PI3 Kinase Inhibitor SF1126 is a Vascular Targeted Conjugate in Phase I Clinical Trials in Solid Tumors and Multiple Myeloma
8. Ardea Biosciences Presents Data Demonstrating Favorable Pharmacokinetics and Efficacy for Mitogen-Activated ERK Kinase (MEK) Inhibitors
9. SuperGen Identifies Lead PIM Kinase Inhibitor, SGI-1776, That Causes Tumor Regression in AML Xenograft Models
10. Latest Cell Publication Describes the Novel Kinase Regulators Using OriGenes Functional Kinome Collection
11. Poniard Pharmaceuticals Licenses Kinase Inhibitors From The Scripps Research Institute
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