MEDI 232 |
| Utilizing Kinex Pharmaceuticals platform technology, MimeticaTM, KXO1 was discovered as a novel small molecule Src tyrosine kinase inhibitor. KXO1 targets the peptide substrate binding site rather than the ATP site wherein most tyrosine kinase inhibitors bind. This unique binding site provides much higher selectivity than is obtained with ATP competitive Src inhibitors. KXO1 inhibits Src kinase activity in whole cells with low nM potency and is >1,000-fold less active against other tyrosine kinases such as EGFRTK, PDGFRTK, JAK1, JAK2, ZAP70 and Lck. KXO1 is also a low nM potency inhibitor of cancer cell growth for a broad range of solid tumor and leukemia cancer cell types in vitro, and is orally effective in animal tumor models. KXO1 has successfully completed preclinical development for oncology applications and will be the first non-ATP competitive Src inhibitor to enter clinical trials. |
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General Oral Session
1:30 PM-4:50 PM, Tuesday, August 21, 2007 BCEC -- 210A, Oral
Division of Medicinal Chemistry |