Taltobulin hydrochloride (Synonyms: HTI-286 hydrochloride; SPA-110 hydrochloride) |
| Katalog-Nr.GC61314 |
Taltobulin-Hydrochlorid (HTI-286-Hydrochlorid), ein synthetisches Analogon des Tripeptids Hemiasterlin, ist ein wirksames Antimikrotubuli-Mittel, das die P-Glykoprotein-vermittelte Resistenz in vitro und in vivo umgeht. Taltobulinhydrochlorid hemmt die Polymerisation von gereinigtem Tubulin, unterbricht die Organisation der Mikrotubuli in Zellen und induziert einen mitotischen Arrest sowie Apoptose.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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].
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]. Cell Proliferation Assay[1] Cell Line: Leukemia CCRF-CEM cell line; ovarian 1A9 cell line; NSCLC A549 and NCI-H1299 cell lines; breast MX-1W and MCF-7 cell lines; colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15 and Moser cell lines; melanoma A375, Lox and SK-Mel-2 cell lines
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]. Animal Model: Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age)[1]
[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.
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