AP 24534

Cat. No. 4274 5 Citations Submit a Review Datasheet / COA / SDS

Pricing	Availability		Qty

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)

Datasheet

Citations (5)

Reviews

Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data 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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Product Datasheets for AP 24534

Certificate of Analysis / Product Datasheet

Safety Datasheet

References for AP 24534

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

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) 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

Gordon et al (2020) A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 583 PMID: 32353859

If you know of a relevant reference for AP 24534, please let us know.

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