Network Version
Taltobulin trifluoroacetate Data Sheet
| Product Name: | Taltobulin trifluoroacetate |
 |
|---|---|---|
| CAS No.: | 228266-41-9 | |
| Cat. No.: | HY-15584A | |
| MWt: | 587.67 | |
| Formula: | C29H44F3N3O6 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 39 mg/mL (66.36 mM) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
|
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate 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]. |
||
1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Web:www.medchemexpress.com