UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively).
CAS：1350547-65-7
分子式：C22H29FN6
分子量：396.5
纯度：98%
存储：Store at -20°C

Background:

UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively). It has antiproliferative activity in vitro against acute lymphoblastic leukemia (ALL) cells (IC50s = 0.5 and 1.2 μM for 697 and Jurkat cell lines, respectively) and inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively). UNC569 activates Akt and ERK1/2 phosphorylation, induces apoptosis, and sensitizes ALL cells to etoposide and methotrexate . In vivo, UNC569 (4 μM) decreases tumor burden by 47.8% relative to vehicle controls in human MYC transgenic zebrafish. UNC569 (10 mg/kg) delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells.