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AP 24534

Cat. No. 4274

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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-ABL^T3151 (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.

Resources

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