博舒替尼(SKI-606)是Src和Abl激酶的有效抑制剂，IC50为1.2 nM和1 nM [1]。

在慢性粒细胞白血病(CML)细胞中，SKI-606抑制Bcr-Abl、Src和Stat5的磷酸化。它还消除了成纤维细胞中v-Abl的表达，并阻止了CML细胞的增殖[2]。在结肠直肠癌细胞中，SKI-606抑制Src自身磷酸化，IC50约为0.25微米，同时抑制Src底物的Tyr (925)磷酸化[3]。SKI-606通过抑制β-连环蛋白与TCF4转录因子的结合来阻断β-连环蛋白的功能，并剂量依赖性地抑制细胞周期蛋白D1。SKI-606增加了β-连环蛋白与E-钙粘蛋白的结合亲和力和粘附力，从而降低了伤口愈合试验中的活动性[4]。

以100 mg/kg的剂量口服SKI-606 5天，导致裸鼠体内大的K562异种移植物完全退化[2]。

产品性质：

Cas No.:380843-75-4

别名:伯舒替尼,SKI-606

化学名: 4-(2,4-dichloro-5-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile

Canonical SMILES:CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC

分子式:C26H29Cl2N5O3

分子量:530.45

溶解度:≥ 26.5mg/mL in DMSO

储存条件:4°C, protect from light

注意事项：

为了您的安全和健康，请穿实验服并戴一次性手套操作。

References:

[1]. Boschelli DH, Ye F, Wang YD, Dutia M, Johnson SL, Wu B, Miller K, Powell DW, Yaczko D, Young M, Tischler M, Arndt K, Discafani C, Etienne C, Gibbons J, Grod J, Lucas J, Weber JM, Boschelli F. 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, Arndt K, Etienne C, Lucas J, Nardin D, Gibbons J, Frost P, Ye F, Boschelli DH, Boschelli F. 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]. Golas JM, Lucas J, Etienne C, Golas J, Discafani C, Sridharan L, Boghaert E, Arndt K, Ye F, Boschelli DH, Li F, Titsch C, Huselton C, Chaudhary I, Boschelli F. SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res. 2005 Jun 15;65(12):5358-64.

[4]. Coluccia AM, Benati D, Dekhil H, De Filippo A, Lan C, Gambacorti-Passerini C. SKI-606 decreases growth and motility of colorectal cancer cells by preventing pp60(c-Src)-dependent tyrosine phosphorylation of beta-catenin and its nuclear signaling. Cancer Res. 2006 Feb 15;66(4):2279-86.