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Ponatinib-d8

Names

[ CAS No. ]:
1562993-37-6

[ Name ]:
Ponatinib-d8

[Synonym ]:
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((2,2,3,3,5,5,6,6-octadeutero-4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide

Biological Activity

[Description]:

Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

[Target]

c-Kit:12.5 nM (IC50)

VEGFR2:1.5 nM (IC50)

FGFR1:2.2 nM (IC50)

PDGFRα:1.1 nM (IC50)


[References]

[1]. O'Hare T, et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell, 2009, 16(5), 401-412.

Chemical & Physical Properties

[ Molecular Formula ]:
C29H19D8F3N6O

[ Molecular Weight ]:
540.60900

[ Exact Mass ]:
540.27000

[ PSA ]:
65.77000

[ LogP ]:
4.40480

Related Compounds