Fluorescent CDK Inhibitors for the Treatment and Diagnosis of Cancer
- Technology Benefits
- Compounds of the invention demonstrate higher % inhibition of CDK2/A and CDK2/E than known CDK2 inhibitor, seliciclibAfluorescent label allow these compounds to be used as both atherapeutic to treat cancer and a diagnostic to detect cancerous cellsand monitor treatmentCell growth inhibition potency (IC50) in certain cancer cell lines is superior to known CDK inhibitors purvanalol and seliciclib
- Detailed Technology Description
- The invention describes promising new fluorescent small moleculepharmaceutical leads for the treatment of cancer by inhibition ofcyclin dependant kinase (CDK). The novel compounds are more potent thanknown CDK inhibitors, purvalanols A and B as well as phase II clinicaldrug candidate, roscovitine (seliciclib). These compounds areespecially potent inhibitors of CDK2 isoforms and effectively arresttumor cells in the G2/M phase. These new compounds may be an effectivenew tool for not only for treating, but also diagnosing cancer andmonitoring cancer therapy.
- *Abstract
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- *Stage of Development
- Growth inhibition, IC50 values were obtained for compounds using the 48hours WST-1 assay in ER negative and ER positive breast cancer celllines. Inhibition of cell cycle protein kinases: CDK1/B, CDK2/A,CDK2/E, CDK3/E and CDK7/CyclinH/MATI, by compounds of the inventionwere compared with commercially available CDK inhibitors purvalanols Aand B and roscovitine. The compounds almost completely inhibited CDK2/Eat nanomolar range. Fluorescence micrographs of breast cancer cellcultures showed that the compounds localized in the cancer cells.
- Country/Region
- USA
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