AP 24534

Name: AP 24534
Brand: Tocris Bioscience
SKU: 4274

Tocris Bioscience a Bio-Techne Brand

Catalog # 4274

Citations (4)

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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

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

Citations for AP 24534 (4)

Showing 1 - 4 of 4 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for AP 24534 include:

Merkulova et al. (2019) Ponatinib treatment promotes arterial thrombosis and hyperactive platelets. Blood Adv. 3:2312
PMID: 31383636
Kim et al. (2018) Voltage-dependent Ca²⁺ channels promote branching morphogenesis of salivary glands by patterning differential growth. Sci Rep. 8:7566
PMID: 29765108
Wong et al. (2014) Production of IL-1β by bone marrow-derived macrophages in response to chemotherapeutic drugs: synergistic effects of dox. and vincri. Cancer Biol Ther. 15:1395
PMID: 25046000
Wong et al. (2013) Small molecule kinase inhibitors block the ZAK-dependent inflammatory effects of dox. Cancer Biol Ther. 14:56
PMID: 23114643

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Product Documents for AP 24534

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.