LY 2784544 - Gandotinib

Potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase (IC50 value 20 and 55 nM for inhibition of JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells, respectively), with no significant inhibitory effect on IL-3 stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50 values >1180 nM) A selective tool for suppression of JAK2V617F-induced myeloproliferative neoplasm (MPN) pathogenesis while minimizing effects on hematopoietic progenitor cells. Moreover, LY2784544 induced apoptosis in inflammatory breast cancer spheres through targeting IL-6-JAK-STAT3 pathway; tested positive in Phase I study in patients with myelofibrosis (MF), polycythemia vera (PV), and essential thrombocythemia (ET).

KEYWORDS: LY 2784544 | supplier | JAK2 Inhibitor | Gandotinib | LY2784544 |CAS [1229236-86-5] | JAK-STATPathway | JAK | Inhibitor | janus kinase | tyrosine kinase | ATP competitive | JAK2V617F | proliferation |  myeloproliferative neoplasm | MNP | apoptosis | inflammatory | myelofibrosis (MF) | polycythemia vera (PV) | essential thrombocythemia (ET)