Ponatinib hydrochloride

BeschreibungIn December 2012, the US FDA approved ponatinib (also referred to as AP 24534) for the treatment of adult patients with chronic phase, accelerated phase, or blast phase chronicmyeloid leukemia (CML). Ponatinib is a pan-Bcr–Abl TKI that blocks both the native (IC50=0.4 nM) and Bcr– AblT315I mutated kinases (IC50=2.0 nM) in addition to othermutated kinases in CML patients. In the Ba/F3 cell proliferation assay, ponatinib inhibits ABL and the T315I Abl mutant with IC50s of 1.2 and 8.8 nM, respectively. Ponatinib was identified by a structure-based drug design approach. Ponatinib binds to the kinase domain in a DFG-out conformation; the ethynyl moiety helps the inhibitor evade the mutant gatekeeper isoleucine residue at position 315. In addition to Abl and the T315I mutant of Abl, ponatinib inhibits VEGFR, PDGFR, FGFR, SRC, KIT, RET, TIE2, FLT3, and EPH receptors at concentrations ranging from0.1 to 20 nM.

VerwendenPonatinib is a tyrosine kinase inhibitors (TKI) and used to treat chronic myeloid leukemia (CML) (1,2,3). Ponatinib is also used in combination with other drugs, such as forskolin, to combat TKI resistance in patient with CML (3), targeted drug in small-cell lung cancer. Potent FAK inhibitor. FGFR/VEGFR/Bcr-Abl inhibitor It is a COVID19-related research product.