Taltobulin (HTI-286) (Synonyms: Taltobulin, SPA 110) |
カタログ番号GC32753 |
トリペプチド ヘミアステリンの合成類似体であるタルトブリン (HTI-286) (HTI-286) は、in vitro および in vivo で P 糖タンパク質を介した耐性を回避する強力な抗微小管剤です。タルトブリン (HTI-286) は、精製チューブリンの重合を阻害し、細胞内の微小管組織を破壊し、有糸分裂停止とアポトーシスを誘導します。
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Cas No.: 228266-40-8
Sample solution is provided at 25 µL, 10mM.
Taltobulin (HTI-286; SPA-110) is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.IC50 value:Target: tubulinin vitro: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure [1]. In all cell lines tested, HTI-286 was a potent inhibitor of proliferation and induced marked increases in apoptosis. Despite similar transcriptomic changes regarding cell death and cell cycle regulating genes after exposure to HTI-286 or docetaxel, array analysis revealed distinct molecular signatures for both compounds [2].in vivo: Intravenous administration of HTI-286 significantly inhibited tumor growth in vivo (rat allograft model) [1]. HTI-286 significantly inhibited growth of PC-3 and LNCaP xenografts and retained potency in PC-3dR tumors. Simultaneous castration plus HTI-286 therapy was superior to sequential treatment in the LNCaP model [2].
[1]. Vashist YK, et al. Inhibition of hepatic tumor cell proliferation in vitro and tumor growth in vivo by taltobulin, a synthetic analogue of the tripeptide hemiasterlin. World J Gastroenterol. 2006 Nov 14;12(42):6771-8. [2]. Hadaschik BA, et al. Targeting prostate cancer with HTI-286, a synthetic analog of the marine sponge product hemiasterlin. Int J Cancer. 2008 May 15;122(10):2368-76.
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