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

在慢性粒細(xì)胞白血病(CML)細(xì)胞中，SKI-606抑制Bcr-Abl、Src和Stat5的磷酸化。它還消除了成纖維細(xì)胞中v-Abl的表達(dá)，并阻止了CML細(xì)胞的增殖[2]。在結(jié)腸直腸癌細(xì)胞中，SKI-606抑制Src自身磷酸化，IC50約為0.25微米，同時(shí)抑制Src底物的Tyr (925)磷酸化[3]。SKI-606通過(guò)抑制β-連環(huán)蛋白與TCF4轉(zhuǎn)錄因子的結(jié)合來(lái)阻斷β-連環(huán)蛋白的功能，并劑量依賴性地抑制細(xì)胞周期蛋白D1。SKI-606增加了β-連環(huán)蛋白與E-鈣粘蛋白的結(jié)合親和力和粘附力，從而降低了傷口愈合試驗(yàn)中的活動(dòng)性[4]。

以100 mg/kg的劑量口服SKI-606 5天，導(dǎo)致裸鼠體內(nèi)大的K562異種移植物完全退化[2]。

產(chǎn)品性質(zhì)：

Cas No.:380843-75-4

別名:伯舒替尼,SKI-606

化學(xué)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

儲(chǔ)存條件:4°C, protect from light

注意事項(xiàng)：

為了您的安全和健康，請(qǐng)穿實(shí)驗(yàn)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.