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TPI-3
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
TPI-3 is a novel small molecule identified as an inhibitor of MKP1 phosphatase. It has demonstrated preclinical activity in sensitizing melanoma and colon cancer cells to existing biotherapeutics and chemotherapeutics. TPI-3 selectively increases MKP1 phosphosubstrates and induces cell death through apoptosis at nanomolar concentrations. It has shown synergistic effects with biotherapeutic IFN alpha 2b in inhibiting melanoma cell growth in vitro and in WM9 xenografts in mice, and also interacted positively with chemotherapeutics, 5-fluorouracil/leucovorin, against MC-26 colon cancer cells in vitro and in mice. It was tolerated as an oral agent in mice.
- Other names
- tyrosine phosphatase inhibitor-3
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