Bafetinib (Synonyms: INNO-406) |
| Catalog No.GC35462 |
바페티닙은 강력하고 경구 활성인 Lyn/Bcr-Abl 티로신 키나제 억제제입니다. Bafetinib은 여러 proapoptotic Bcl-2 homology(BH)3-only protein(Bim, Bad, Bmf, Bik)의 활성을 증가시키고 Bcl-2 family에 의해 조절되는 고유의 세포사멸 경로를 통해 Ph+ 백혈병 세포에서 세포사멸을 유도합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 859212-16-1
Sample solution is provided at 25 µL, 10mM.
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Bafetinib is a potent and selective dual inhibitor of Bcr-Abl/Lyn tyrosine kinase with IC50 values of 5.8nM and 19nM, respectively [1].
Bafetinib is a specific dual Abl-Lyn inhibitor. For 79 other tyrosine kinases, 0.1μM bafetinib can inhibit 4 of these enzymes including Abl, Abl-related gene, Fyn and Lyn. Bafetinib can block the autophosphorylation of Bcr-Abl. In K562 and 293T cells transfected with wt Bcr-Abl, bafetinib shows inhibition with IC50 values of 11nM and 22nM, respectively. In the in vitro kinase assays, bafetinib shows inhibition of a variety of Abl kinase mutants such as M244V, G250E, Y253F and F317L. It has no effect on T315I in vitro. Bafetinib also suppresses the growth of Bcr-Abl–positive leukemic cell lines including K562, KU812 and BaF3/wt. The BaF3/E255K cells are also sensitive towards bafetinib. Moreover, bafetinib is highly potent to inhibit tumor growth in murine tumor models [1].
References:
[1] Kimura S, Naito H, Segawa H, et al. NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood, 2005, 106(12): 3948-3954.
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