AP 24534

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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)
Citations (5)

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-AblT3151 (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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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
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5 Citations for AP 24534

Citations are publications that use Tocris products. Selected citations for AP 24534 include:

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

Kim et al (2018) Voltage-dependent Ca2+ channels promote branching morphogenesis of salivary glands by patterning differential growth. Sci Rep 8 7566 PMID: 29765108

Alastair D et al (2021) Impact of Type II LRRK2 inhibitors on signaling and mitophagy. Biochem J 478 3555-3573 PMID: 34515301

Merkulova et al (2019) Ponatinib treatment promotes arterial thrombosis and hyperactive platelets. Blood Adv 3 2312 PMID: 31383636

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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