产品
编 号：F283354
分子式：C27H43N3O4
分子量：473.65
分子式：C27H43N3O4
分子量：473.65
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 228266-40-8
产品详情
生物活性：
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.
体内研究：
TaltobuLin (HTI-286; 1.6 mg/kg; iv) 抑制无胸腺 nu/nu 雌性小鼠中人肿瘤异种移植物 (例如，HCT-15、DLD-1、MX-1W 和 KB-8-5) 的肿瘤生长。 TaltobuLin (HTI-286；3 mg/kg；口服灌胃) 在具有 Lox 黑色素瘤异种移植物和 KB-3-1 表皮样异种移植物模型的无胸腺 nu/nu 雌性小鼠中抑制率分别为 97.3% 和 82%。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 天) 抑制 18 种肿瘤细胞系 (白血病、卵巢、NSCLC、乳腺癌、结肠和黑色素瘤细胞系) 的生长，平均 IC50 为 2.5±2.1 nM，中值为 1.7 nM。
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.
体内研究：
TaltobuLin (HTI-286; 1.6 mg/kg; iv) 抑制无胸腺 nu/nu 雌性小鼠中人肿瘤异种移植物 (例如，HCT-15、DLD-1、MX-1W 和 KB-8-5) 的肿瘤生长。 TaltobuLin (HTI-286；3 mg/kg；口服灌胃) 在具有 Lox 黑色素瘤异种移植物和 KB-3-1 表皮样异种移植物模型的无胸腺 nu/nu 雌性小鼠中抑制率分别为 97.3% 和 82%。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 天) 抑制 18 种肿瘤细胞系 (白血病、卵巢、NSCLC、乳腺癌、结肠和黑色素瘤细胞系) 的生长，平均 IC50 为 2.5±2.1 nM，中值为 1.7 nM。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备