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  • CE-245677
CE-245677的可视化放大

CE-245677

CE-245677是一种有效的,可逆的Tie2和TrkA/B抑制剂,在细胞体系下,IC50值分别为4.7和1nM。

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CE-245677的二维码
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  • 货号: ajcx12842
  • CAS: 717899-97-3
  • 别名:
  • 分子式: C24H22Cl2N6O3
  • 分子量: 513.38
  • 纯度: >98%
  • 溶解度: DMSO: 125 mg/mL (243.48 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.


CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50 of 4.7 and 1 nM, and displays >100x selectivity against a number of other angiogenic receptor tyrosine kinases, such as KDR, PDGFR, FGFR[1].


CE-245677 shows good oral absorption in in vivo rat PK studies (F=80%)[1].


[1]. Susan LaGreca, et al. Identification of selective, orally active Tie2 kinase inhibitors and discovery of CE-245,677 and PF-371,989. Cancer Research. AACR Annual Meeting-Apr 14-18, 2007.

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