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CEP-11981

Names

[ CAS No. ]:
856691-93-5

[ Name ]:
CEP-11981

[Synonym ]:
unii-j8ay0z4cbp

Biological Activity

[Description]:

CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

[In Vitro]

CEP-11981(1μM, 72 h) 可以显著抑制 RT4 细胞生长[1]。

[In Vivo]

CEP-11981（2.5 mg/kg、5 mg/kg 或 10 mg/kg，口服强饲法，每天，每周 5 天，持续两周）在 RT4 人 UC 肿瘤小鼠模型中，与对照相比显着抑制了 UC 异种移植物的生长，而小鼠本身重量没有变化[1]。

[References]

[1]. Weiguo Jian, et al. The angiopoietin-TIE2 pathway is a potential therapeutic target in urothelial carcinoma. Anticancer Res. 2014 Jul;34(7):3377-82.  

Chemical & Physical Properties

[ Molecular Formula ]:
C28H27N7O

[ Molecular Weight ]:
477.56000

[ Exact Mass ]:
477.22800

[ PSA ]:
104.01000

[ LogP ]:
4.07950

Related Compounds