Taltobulinhydrochloride(HTI-286hydrochloride)是一种合成的三肽半胱氨酸类似物，Taltobulin是一种有效的抗微管剂(antimicrotubule)，可在体内外规避P-糖蛋白介导的耐药性。Taltobulinhydrochloride抑制纯化的微管蛋白聚合，破坏细胞中的微管组织，并诱导有丝分裂停滞以及凋亡(apoptosis)。
货号:ajcx31542
CAS:N/A
分子式:C27H44ClN3O4
分子量：510.11
溶解度:DMSO: ≥ 100 mg/mL (196.04 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.