AP 24534

Product Description

AP 24534 is a 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. Identified as targeting human host proteins that interact with SARS-CoV-2.

Solubility

Preparing Stock Solutions for AP 24534

The following data is based on the product molecular weight 532.56

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.88 mL	9.39 mL	18.78 mL
5 mM	0.38 mL	1.88 mL	3.76 mL
10 mM	0.19 mL	0.94 mL	1.88 mL
50 mM	0.04 mL	0.19 mL	0.38 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Gordon A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 2020 PMID: 32353859
• Huang 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) J.Med.Chem. 2010 PMID: 20513156
• Gozgit Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol.Cancer Ther. 2011 PMID: 21482694
• O'Hare AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 2009 PMID: 19878872