BBT594

BBT594 (NVP-BBT594) is a potent and selective inhibitor of RET and JAK2. BBT594 impairs "glial-derived neurotrophic factor" (GDNF)-RET signaling and GDNF-dependent growth in specific in vitro models. Direct inhibition of GDNF-RET signaling by BBT594 in ER+ breast cancer cells enhances the sensitivity to aromatase inhibitor (AI) treatment and reverts AI resistance. In murine models, the IC50 of BBT594 on JAK2 inhibition varies between 8nM - 29nM, depending on the cell model and abundant JAK2 mutations.