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Taltobulin(HTI-286)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Taltobulin(HTI-286)图片
CAS NO:228266-40-8
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
Taltobulin (HTI-286) (HTI-286) 是一种合成的三肽 hemiasterlin 类似物，是一种有效的抗微管药物，可在体外和体内规避 P-糖蛋白介导的耐药性。 Taltobulin (HTI-286) 抑制纯化的微管蛋白的聚合，破坏细胞中的微管组织，并诱导有丝分裂停滞以及细胞凋亡。
Cas No.228266-40-8
别名N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺,HTI-286; SPA-110
Canonical SMILESCC(C)(C)[C@H](NC([C@H](C(C)(C1=CC=CC=C1)C)NC)=O)C(N([C@@H](C(C)C)/C=C(C(O)=O)\C)C)=O
分子式C27H43N3O4
分子量473.65
溶解度DMSO : ≥ 100 mg/mL (211.13 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.