| 产品描述： | Taltobulin (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. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis |
| 靶点： |
Traditional Cytotoxic Agents;MicrotubuleAssociated |
| 体内研究： |
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. 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 Animal Model: Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age) Dosage: 1.6 mg/kg Administration: Administered i.v.;for 35 days Result: Growth of Lox tumors was inhibited by 96-98% on day 12 compared with vehicle-treated controls.Growth of KB-8-5 tumors was inhibited by 84% on day 14 compared with vehicle-treated controls.Growth of MX-1W tumors was inhibited by 97% compared with vehicle-treated controls.Growth of DLD-1 and HCT-15 tumors was inhibited by 80 and 66%, respectively. |
| 参考文献： |
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. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
2-8℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.111 ml |
10.556 ml |
21.113 ml |
| 5 mM |
0.422 ml |
2.111 ml |
4.223 ml |
| 10 mM |
0.211 ml |
1.056 ml |
2.111 ml |
| 50 mM |
0.042 ml |
0.211 ml |
0.422 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京