CPL423 is a potent selective TAM family of receptor tyrosine kinases (TYRO3, AXL, MERTK) and FLT3 inhibitor with IC50 of MERTK (0.47 nM) and FLT3 (0.94 nM), inhibits AXL and TYRO3 with IC50 of 2.15 and 6.73 nM, respectively.
CPL423 demonstrates markedly reduced activity against other kinases, with IC50 values of 60.35 nM for PDGFRβ, 71.91 nM for TrkA, 221.90 nM for TrkC, and 13900 nM for TrkB.
CPL423 exhibits potent, dose-dependent cytotoxic activity. The IC50 was 5.7 nM in MOLM-13 cells and 7.92 nM in MV4-11 cells.
CPL423 reduces cell viability with an IC50 of 388.1 nM in A375 melanoma cell line.
CPL423 reduces MERTK phosphorylation (pMERTK) in a dose-dependent manner across 1–250 nM in MERTK-stable Ba/F3 cells, reduces phosphorylation of AKT and ERK.
CPL423 reduces the phagocytic capacity of bone marrow-derived mouse dendritic cells (BMDCs).
CPL423 (30 to 50 mg/kg, orally, once daily (QD)) demonstrates antitumor activity in MOLM-13 xenograft model.