AZ12672857

Names

[ Name ]:
AZ12672857

Biological Activity

[Description]:

AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM)[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

[Target]

EP4:1.3 nM (IC50)

Src

[In Vitro]

AZ12672857 shows only modest inhibition of CYP P450 (IC50=5 μM against 2C9 and 3A4, >10 μM against 1A4, 2D6 and 2C19). AZ12672857 inhibits p-KDR in HUVEC with an IC50 of 240 nM and inhibits p-PDGFR-βin MG63 cell line with an IC50 of 58 nM[1].

[References]

[1]. Bardelle C, et al. Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors. Bioorg Med Chem Lett. 2010;20(21):6242-6245.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₃₀N₈O₂

[ Molecular Weight ]:
486.57

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds

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