Taltobulin hydrochloride is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.

The growth of 18 tumor cell lines (leukemia, ovarian, NSCLC, breast, colon, and melanoma cell lines) inhibited by Taltobulin (HTI-286; 0.2-7.3 nM; 3 days)(with an average IC50 of 2.5±2.1 nM and a median value of 1.7 nM).

In athymic nu/nu female mice, Taltobulin (HTI-286; 1.6 mg/kg i.v.) inhibits the growth of human tumor xenografts (e.g., HCT-15, DLD-1, MX-1W, and KB-8-5) . Taltobulin (HTI-286; 3 mg/kg; p.o. gavage) inhibits growth by 97.3 % and 82% in athymic nu/nu female mice with Lox melanoma xenografts and KB-3-1 epidermoid xenograft model, respectively.

T13073L

C27H44ClN3O4

510.11

HTI-286 hydrochloride;Taltobulin hydrochloride;SPA-110 hydrochloride;Taltobulin hydrochloride (228266-40-8 free base)

DMSO:100 mg/mL (196.04 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years