产品
编 号：F283355
分子式：C29H44F3N3O6
分子量：587.67
分子式：C29H44F3N3O6
分子量：587.67
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 228266-41-9
产品详情
生物活性：
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.
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.
体外研究：
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.
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.
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.
体外研究：
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.
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