GDC-0339 is a potent, orally bioavailable, and well-tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM, and 0.02 nM for Pim1, Pim2, and Pim3, respectively. It is being explored as a potential treatment for multiple myeloma.
- Potent, orally bioavailable, and well-tolerated pan-Pim kinase inhibitor.
- Discovered as a potential treatment for multiple myeloma.
- Cytostatic with an IC50 of 0.1 μM for MM.1S cells.
- Induces a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases.
- Efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models.