Catalog No.: PC-21414Not For Human Use, Lab Use Only.
Itacnosertib (TP-0184) is a novel potent, selective inhibitor of type I bone morphogenetic protein (BMP) receptor ACVR1 (activin A receptor-type 1, ALK2) and FLT3 with IC50 of 8.0 nM (ALK2).
Itacnosertib (TP-0184) is a novel potent, selective inhibitor of type I bone morphogenetic protein (BMP) receptor ACVR1 (activin A receptor-type 1, ALK2) and FLT3 with IC50 of 8.0 nM (ALK2).
TP-0184 binds to both ACVR1 and FLT3 with high affinity and inhibits FLT3/ACVR1 downstream signaling.
TP-0184 selectively caused growth arrest in FLT3-mutated AML cell lines.
Treatment with TP-0184 or in combination with BCL2 inhibitor, venetoclax dramatically inhibited leukemia growth in FLT3-mutated AML cell lines and patient-derived xenograft models in a dose-dependent manner.
