AP 24534

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Cat.No. 4274 - AP 24534 | C29H27F3N6O | CAS No. 943319-70-8
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 (2)
Reviews
Literature

Biological Activity

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.

Compound Libraries

AP 24534 is also offered as part of the Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 532.56. Batch specific molecular weights may vary from batch to batch due to solvent 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

Safety Datasheet

References

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


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

View Related Products by Product Action

View all Abl Kinase Inhibitors

Keywords: AP 24534, AP 24534 supplier, AP24534, BCR-ABL, kinases, mutations, break, point, cluster, c-abl, abelson, multikinase, inhibitors, inhibits, vegfr, fgfr, pdgfralpha, pdgfra, pdgfrα, potent, Ponatinib, Abl, Kinase, VEGFR, FGFR, PDGFR, 4274, Tocris Bioscience

2 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 doxorubicin and vincristine. Cancer Biol Ther 15 1395 PMID: 25046000

Wong et al (2013) Small molecule kinase inhibitors block the ZAK-dependent inflammatory effects of doxorubicin. Cancer Biol Ther 14 56 PMID: 23114643


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Literature in this Area

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