AZ12672857 |
| Katalog-Nr.GC60611 |
AZ12672857 ist ein oral aktiver Inhibitor von EphB4 (IC50=1,3 nM) und Src-Kinasen. AZ12672857 zeigt eine gute Hemmung der Proliferation von c-Src-transfizierten 3T3-Zellen (IC50 = 2 nM) sowie eine Autophosphorylierung von EphB4 in transfizierten CHO-K1-Zellen (IC50 = 9 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 945396-55-4
Sample solution is provided at 25 µL, 10mM.
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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].
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].
[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.
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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