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CE-245677

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Chemical Structure| 717899-97-3 同义名 : -
CAS号 : 717899-97-3
货号 : A429803
分子式 : C24H22Cl2N6O3
纯度 : 97%
分子量 : 513.376
MDL号 : MFCD31657440
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(233.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The Tie receptor tyrosine kinases play an important role in the development of endothelial tissues. The Tie receptors (Tie1 and Tie2) and their ligands (angiopoietins) are highly involved in the survival and functional integrity of the vasculature. CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with IC50 values of 4.7 and 1nM, respectively. It showed over 1000-fold selectivity against other angiogenic receptor tyrosine kinases, including kinase insert domain receptor, platelet-derived growth factor receptor, and fibroblast growth factor receptors, and gene family panels. CE-245677 also exhibited good oral bioavailability (F=80%) in rat pharmacokinetic study[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.48mL

3.90mL

1.95mL
参考文献

[1]Identification of selective, orally active Tie2 kinase inhibitors and discovery of CE-245,677 and PF-371,989