| Description | 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. |
| In vitro | 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 vivo | 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. |
| Synonyms | SPA-110 hydrochloride, Taltobulin hydrochloride, HTI-286 hydrochloride |
| molecular weight | 510.11 |
| Molecular formula | C27H44ClN3O4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (196.04 mM) |
| References | 1. Loganzo F, et al. HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Cancer Res. 2003 Apr 15;63(8):1838-45. |