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Taltobulin hydrochloride Data Sheet
| Product Name: | Taltobulin hydrochloride |
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| CAS No.: | ||
| Cat. No.: | HY-15584B | |
| MWt: | 510.11 | |
| Formula: | C27H44ClN3O4 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 100 mg/mL (196.04 mM) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis[1].
In Vitro: Taltobulin (HTI-286; 0.2-7.3 nM; 3 days) inhibits the growth of 18 tumor cell lines (leukemia, ovarian, NSCLC, breast, colon, and melanoma cell lines) with an average IC50 of 2.5±2.1 nM and a median value of 1.7 nM[1].
In Vivo: 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) in athymic nu/nu female mice[1]. 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[1]. |
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