AP 24534

Name: AP 24534
Brand: Tocris Bioscience
SKU: 4274

Tocris Bioscience, part of Bio-Techne | Catalog # 4274

Citations (4)

COA / SDS

Potent multi-kinase and pan-Bcr-Abl inhibitor

Key Product Details

Description:	Potent multi-kinase and pan-Bcr-Abl inhibitor
Alternative 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
Purity:	≥98% (HPLC)
Molecular Weight:	532.56

View Full Technical Details for AP 24534

Technical Data
Citations

Biological Activity for AP 24534

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.

Technical Data for AP 24534

M. Wt	532.56
Formula	C₂₉H₂₇F₃N₆O
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	943319-70-8
PubChem ID	24826799
InChi Key	PHXJVRSECIGDHY-UHFFFAOYSA-N
Smiles	CC1=CC=C(C(NC4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4)=O)C=C1C#CC2=CN=C3N2N=CC=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for AP 24534

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	53.26	100
	ethanol	26.63	50

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for AP 24534

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