Catalog No.: PC-35619Not For Human Use, Lab Use Only.
BPR1J373 is a potent, orally available multitargeted kinase inhibitor, potently inhibits FLT3, c-KIT, VEGFR1-3, Aurora A, PDGFRα, PDGFRβ, RET, and SRC with IC50 values of <100 nM.
BPR1J373 is a potent, orally available multitargeted kinase inhibitor, potently inhibits FLT3, c-KIT, VEGFR1-3, Aurora A, PDGFRα, PDGFRβ, RET, and SRC with IC50 values of <100 nM.
BPR1J373 inhibits cell proliferation of myeloid leukemia cell lines and primary leukemia cells with constitutively activated c-KIT (KG-1, K562 cell with IC50 of 45 and 49 nM).
BPR1J373also suppresses c-KIT in AML cell lines and primary AML cells; induces apoptosis by mitochondrial intrinsic pathway through upregulation of proapoptotic proteins Bax and Bak and caspase 8 and 9 activation in Kasumi-1 cells, induces cell-cycle arrest for c-KIT–driven leukemia cells via targeting different signals.
BPR1J373 effectively suppressed Kasumi-1 cells in xenograft mouse model, effectively suppresses c-KIT phosphorylation of D816V mutation.
