Ponatinib Hydrochloride

Product Name:

Ponatinib Hydrochloride

Synonyms:

AP24534 Mono-hydrochloride;Ponatinib Mono-hydrochloride;3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide hydrochloride;Ponatinib hydrochloride;Ponatinib-HCl;AP24534-HCl;1114544-31-8

CAS:

MF:

C29H28ClF3N6O

MW:

569.02

EINECS:

1592732-453-0

Product Categories:

 

Mol File:

1114544-31-8.mol

 

Ponatinib Hydrochloride Chemical Properties

 

Safety Information

MSDS Information

 

Ponatinib Hydrochloride Usage And Synthesis

Description

In 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– Abl^T315I 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 IC_50s 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.

Originator

Ariad (United States)

Brand name

Iclusig