货号 | 12030-5mg |
描述 | The non-receptor tyrosine kinases c-Src and Abl have important roles in cell signaling and cancer. Bosutinib is best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.0 nM, respectively).1,2 Consistent with this action, bosutinib can be effective in regulating tumor growth and differentiation.3,4 Bosutinib is best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.0 nM, respectively).1,2 Consistent with this action, bosutinib can be effective in regulating tumor growth and differentiation.3,4 Bosutinib also inhibits, at nanomolar concentrations, other members of the Src family (e.g., Yes, Fgr, Lck, Fyn), as well as members of the TEC family, and certain other kinases.5 These actions extend the usefulness of this compound to cancers beyond those involving Src and Abl.6 |
别名 | SKI 606; |
供应商 | Cayman |
应用文献 | |
1.Boschelli, D.H.,Ye, F.,Wang, Y.D., et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. Journal of Medicinal Chemistry 44, 3965-3977 (2001). 2.Golas, J.M.,Arndt, K.,Etienne, C., 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 Research 63(2), 375-381 (2003). 3.Golas, J.M.,Lucas, J.,Etienne, C., et al. SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Research 65(12), 5358-5364 (2005). 4.Hebbard, L.,Cecena, G.,Golas, J., et al. Control of mammary tumor differentiation by SKI-606 (bosutinib). Oncogene 30(3), 301-312 (2011). 5.Remsing Rix, L.L.,Rix, U.,Colinge, J., et al. Global target profile of the kinase inhbitor bosutinib in primary chronic myeloid leukemia cells. Leukemia 23, 477-485 (2009). 6.Gleixner, K.V.,Mayerhofer, M.,Cerny-Reiterer, S., et al. KIT-D816V-independent oncogenic signaling in neoplastic cells in systemic mastocytosis: Role of Lyn and Btk activation and disruption by dasatinib and bosutinib. Blood 118(7), 1885-1898 (2011). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 530.5 |
分子式 | C26H29Cl2N5O3 |
CAS号 | 380843-75-4 |
稳定性 | ≥ 2 years |
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