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AZ12672857
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZ12672857图片
CAS NO:945396-55-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
AZ12672857是具有口服活性的EphB4(IC50=1.3nM)和Src激酶的抑制剂。AZ12672857抑制c-Src转染3T3细胞的增殖(IC50=2nM)和抑制转染CHO-K1细胞中的EphB4自磷酸化(IC50=9nM)。
Cas No.945396-55-4
Canonical SMILESCN(C1=CC=CC2=C1C=NN2)C3=NC(NC4=CC(N5CCOCC5)=CC(N6CCOCC6)=C4)=NC=C3
分子式C26H30N8O2
分子量486.57
溶解度DMSO: 25 mg/mL (51.38 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.