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Ponatinib

Chemical Structure : Ponatinib

CAS No.: 943319-70-8

Ponatinib (AP 24534, AP24534, AP-24534)

Catalog No.: PC-42862Not For Human Use, Lab Use Only.

Ponatinib (AP 24534) is a potent, orally active pan-inhibitor of BCR-ABL kinase with IC50 of 0.37 and 2.0 nM for ABL and mutant ABLT315I, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Ponatinib (AP 24534) is a potent, orally active pan-inhibitor of BCR-ABL kinase with IC50 of 0.37 and 2.0 nM for ABL and mutant ABLT315I, respectively.
Ponatinib retains high potency against other ABL mutants Q252H, Y253F, M351T and H396P (IC50s<0.5 nM), also inhibits c-Src, Lyn, c-KIT, VEGFR2, FGFR1, PDGFRα (IC50s=0.2-5 nM).
Ponatinib inhibits the growth of cells expressing native or mutant BCR-ABL (IC50s=0.5–36 nM).
Ponatinib suppresses BCR-ABL(T315I)-driven tumor growth in mice, and completely abrogated resistance in cell-based mutagenesis screens.

Physicochemical Properties

M.Wt 532.5595
Formula C29H27F3N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 50 mg/mL

Chemical Name/SMILES

Benzamide, 3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-

References

1. Gozgit JM, et al. Mol Cancer Ther. 2011 Jun;10(6):1028-35.

2. Huang WS, et al. J Med Chem. 2010 Jun 24;53(12):4701-19.

3. O'Hare T, et al. Cancer Cell. 2009 Nov 6;16(5):401-12.

4. Gozgit JM, et al. Mol Cancer Ther. 2012 Mar;11(3):690-9.

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