SYHA1813 is a potent dual inhibitor of CSF1R and VEGFR with IC50 of 19.3, 2.8, 0.3, and 4.3 nM for CSF1R, VEGFR1, 2, and 3, respectively.
SYHA1813 shows selectivity against a panel of 328 kinases at 0.1 uM. binds to the ATP binding site of VEGFR-2 or CSF1R in a "DFG-out" conformation.
SYHA1813 influences the cell viability and differentiation of BMDMs and suppresses angiogenesis, efficiently blocks the CSF1R activation and downstream signaling transduction induced by the TCM.
SYHA1813 dose-dependently inhibited the CSF1-stimulated cell viability of bone marrow-derived macrophages (BMDMs) with IC50 of 90 nM, inhibited the VEGF-mediated proliferation of HUVEC with IC50 of 13 nM.
SYHA1813 blocks tumor growth in GBM xenograft models including TMZ insensitive tumor by inhibiting VEGFR and CSF1R.
SYHA1813 effectively crosses the BBB and prolongs the survival time of mice with intracranial GBM tumors.