Catalog Number: 4274
Alternate Names: Ponatinib
Chemical Name: 3-(2-Imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-benzamide
Biological Activity
Potent multi-kinase and pan-Bcr-Abl inhibitor. Displays potent activity against cell lines expressing native Bcr-Abl or Bcr-AblT3151 (IC50 values are 0.37 and 2.0 nM respectively); also inhibits other Abl kinase domain mutants at nanomolar potencies. Exhibits inhibitory activity against PDGFRα, c-Src and c-Kit (IC50 values are 1.1, 5.4 and 12.5 nM respectively); potently inhibits FGFR and VEGFR family kinases. Orally active.
Technical Data
  • M.Wt:
    532.56
  • Formula:
    C29H27F3N6O
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    943319-70-8
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)-methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-Abelson (BCR-ABL)
    Huang et al.
    J.Med.Chem., 2010;53:4701
  2. Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies.
    Gozgit et al.
    Mol.Cancer Ther., 2011;10:1028
  3. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.
    O'Hare et al.
    Cancer Cell, 2009;16:401

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