945396-55-4

945396-55-4 structure

Name: AZ12672857
Chemical Name: AZ12672857
CAS Number: 945396-55-4
Molecular Formula: C₂₆H₃₀N₈O₂
Molecular Weight: 486.57
Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
Create Date: 2020-11-20 20:31:06
Modify Date: 2024-01-07 18:16:54
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].

Name	AZ12672857

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.

Molecular Formula	C₂₆H₃₀N₈O₂
Molecular Weight	486.57

Hazard Codes	Xi