Ponatinib, Free Base (AP-24534, Iclusig, CAS 943319-70-8), >99%

LC Laboratories' Product Number P-7022 - Ponatinib, Free Base (AP-24534, Iclusig, CAS 943319-70-8), >99% - for research use only. Ponatinib, also known as AP24534, is a multi-targeted tyrosine kinase inhibitor and is active against T315I and other BCR-ABL mutants. Ponatinib inhibited native BCR-ABL (IC50 = 0.37 nM) and the mutants with IC50 values of 2 nM (T315I); 0.44 nM (Q252H); 0.3 nM (Y253F); 0.3 nM (M351T); and 0.34nM (H396P) in biochemical assays. It also inhibited the growth of Ba/F3 cells with IC50 values of 0.5 nM (Native BCR-ABL), 11 nM (T315I), 2.2 nM (Q252H), 2.8 nM (Y253F), 1.5 nM (M351T), and 1.1 nM (H396P). It suppressed BCR-ABL(T315I)-driven tumor growth in mice and completely overcame resistance in cell-based mutagenesis screens. Ponatinib inhibited FGFR-mediated signaling and viability with IC50 values <40 nM in Ba/F3 cells engineered to express activated FGFR 1-4, with substantial selectivity over parental Ba/F3 cells. It also inhibited FGFR-mediated signaling with IC50 values <40 nM and inhibited cell growth with GI50 values of 7 to 181 nM in a panel of 14 cell lines representing multiple tumor types (endometrial, bladder, gastric, breast, lung, and colon) and containing dysregulated FGFRs. Ponatinib treatment reduced tumor growth and inhibited signaling in all three mouse tumor models examined. In a pivotal phase 2 trial, ponatinib had substantial activity in heavily pretreated patients and those with refractory T315I. Response rates continued to improve with longer follow-up. Ponatinib is the active ingredient in the drug product sold under the trade name Iclusig®. This drug is currently approved in at least one country for use in patients with chronic myeloid leukemia (CML) and Philadelphia chromosome positive (Ph+) acute lymphoblastic leukemia (ALL). NOTE: THE PONATINIB, FREE BASE RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT ICLUSIG®, AND IS NOT FOR HUMAN USE. Related CAS numbers: 1114544-31-8 for the Ponatinib HCl salt. Another CAS number previously assigned to Ponatinib, Free Base, namely 952306-26-2, has been deleted by CAS and is no longer in use.

• Supplier: LC Laboratories
• Product #: P-7022
• Sku #: P-7022_200mg