Taltobulin盐酸盐是Hemiasterlin类似物, 微管蛋白抑制剂和抗体药物偶连体毒素组分 (ADCs cytotoxin)。
Description | Taltobulin hydrochloride is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin. IC50 value: Target: tubulin in vitro: HTI-286 significantly inhibits proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L). Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure [1]. In all cell lines tested, HTI-286 is 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 inhibits tumor growth in vivo (rat allograft model) [1]. HTI-286 significantly inhibits growth of PC-3 and LNCaP xenografts and retained potency in PC-3dR tumors. Simultaneous castration plus HTI-286 therapy is superior to sequential treatment in the LNCaP model [2]. | ||||||||||||||||
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Solvent & Solubility | In Vitro: 10 mM in DMSO Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References | |
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