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伯舒替尼Bosutinib(SKI-606) Src/Abl抑制剂|CAS 380843-75-4(53267ES)

Bosutinib伯舒替尼
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Bosutinib (SKI-606, SKI606),也称伯舒替尼,是一种新型的双重酪氨酸激酶Src/Abl抑制剂,IC50分别为1.2 nM和1 nM,表现出抗癌活性,常用于治疗慢性粒细胞性白血病(CML)。此外,Bosutinib能促进自噬,抑制ERK和STAT3的磷酸化。

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参考文献

  1. Boschelli DH, et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem. 2001 Nov 8;44(23):3965-77.
  2. Golas JM, et al. SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res. 2003 Jan 15;63(2):375-81.
  3. Vultur A, et al. SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells. Mol Cancer Ther. 2008 May;7(5):1185-94.

 

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