tcsc5091 Taltobulin (hydrochloride)

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].