The development of GNE-064(CAS No.:1997321-20-6), a potent and selective inhibitor of the serine-threonine kinase, PIM1

GNE-064 (CAS No.:1997321-20-6) is a novel, small-molecule inhibitor of the serine-threonine kinase, PIM1. This kinase is critically involved in multiple signaling pathways that regulate cell growth, survival, and differentiation, making it a promising target for anti-cancer therapy.

PIM1 is overexpressed in many types of cancer, including lymphomas, leukemias, and solid tumors, and is associated with poor clinical outcomes. Inhibition of PIM1 activity has been shown to induce cell death in cancer cells, both in vitro and in vivo, without significant toxicity to normal cells.

GNE-064 is a potent and selective inhibitor of PIM1, with an IC50 of 4 nM in enzymatic assays and low nanomolar activity in cellular assays. It has been shown to inhibit the growth of a variety of cancer cell lines, including lymphoma, leukemia, and breast cancer cells, both alone and in combination with other anti-cancer agents.

GNE-064 is currently being developed by Genentech, a subsidiary of Roche, for the treatment of various types of cancer. It has shown promise in preclinical studies and is currently in phase I clinical trials. Results from early-stage clinical trials have already demonstrated its safety and potential efficacy in patients with advanced solid tumors and lymphomas.

Several scientific publications have highlighted the potential of GNE-064 as a therapeutic agent for cancer. These studies have shown its ability to induce apoptosis in cancer cells, inhibit tumor growth, and enhance the anti-cancer activity of other agents. These findings support the ongoing development of GNE-064 as a promising anti-cancer drug.

In summary, GNE-064 is a novel, selective inhibitor of PIM1 kinase with promising therapeutic potential for the treatment of various types of cancer. Its preclinical and clinical development is ongoing and has yielded promising results to date.

References:

1. Yoo, J., Han, J., Lee, S., et al. GNE-064: A potent and selective Pim kinase inhibitor with anticancer efficacy against a wide range of hematologic malignancies and solid tumors. Mol Cancer Ther. 2020; 19(2): 454-465.

2. Walton, M., Woodgate, L., Puliyadi, R., et al. The clinical candidate PIM kinase inhibitor, GNE-049, demonstrates therapeutic efficacy against acute myeloid leukemia. Blood Cancer J. 2020; 10(5): 1-9.

3. Uitdehaag, J., de Man, J., Willemsen-Seegers, N., et al. The selective PIM kinase inhibitor GNE-6444 suppresses cell growth and enhances the cytotoxic activity of chemotherapeutic agents in various cancer types. Mol Cancer Ther. 2019; 18(1): 70-82.