AP 24534

Cat. No. 4274

AP 24534 C29H27F3N6O [943319-70-8]

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Alternative Name: 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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

O'Hare et al (2009) AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 16 401. PMID: 19878872.

Huang et al (2010) 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) kinase including the T3151 mutant. J.Med.Chem. 53 4701. PMID: 20513156.

Gozgit et al (2011) Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol.Cancer Ther. 10 1028. PMID: 21482694.

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Keywords: AP 24534, supplier, AP24534, BCR-ABL, kinases, mutations, break, point, cluster, c-abl, abelson, multikinase, inhibitors, vegfr, fgfr, pdgfralpha, pdgfra, pdgfrα, potent, Ponatinib, Tocris Bioscience, Abl Kinase Inhibitors

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