TTT-28  

促销价¥{{model.attbuying.price}}

市场价¥0.00

累计销量0 累计评价0 人评论

别称 {{model.alias}}
中文名称 {{model.name}}
英文名称 {{model.enname}}
品牌 {{model.brand}}
CAS {{model.cas}}
分子式
分子量 {{model.molecularweight}}
MDL {{model.mdl}}
货号 {{model.procode}}
数量

+ -

库存{{model.attbuying.number}}
包装规格:100mg in glass bottle
产品描述:基本信息 产品编号: T11028  产品名称: TTT-28 CAS: 1609138-51-3   储存条件 粉末 -20℃ 四年 分子式: C31H31N3O6S 溶于液体 -80℃ 二年 分子量: 573.66     化学名:    Solubility (25°C):   体外:   DMSO   Ethanol   Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   生物活性 产品描述 一种噻唑-缬氨酸肽模拟物,高效ABCB1(P-gp/MDR1)选择性抑制剂,低毒性。TTT-28通过选择性阻断ATP结合盒亚家族B成员1(ABCB1)的外排功能,逆转ABCB1介导的多药耐药性(MDR)。 靶点 P-glycoprotein   体外研究 TTT-28 (0-100μM;72 hours) reverses ABCB1-mediated MDR in drug selected SW620/Ad300 cells and transfected HEK293/ABCB1 cells;the IC50s of TTT-28 in CCD-18Co,SW620 and SW620/Ad300 cells are 213.4±11.0μM,89.4±3.9μM and 92.0±5.0μM,respectively.TTT-28 (10μM;2 hours) raises the ABCB1-mediated MDR and increased the accumulation of [3H]-paclitaxel in ABCB1 overexpressing cells.TTT-28 (10μM;0-72 hours) does not interfer with the expression level and localization of ABCB1,it results from blocking the efflux function of ABCB1.TTT-28 (0-40μM;2 hours) interacts at the drug-substrate-binding site and actives the ATPase activity of ABCB1 in a concentration-dependent fashion. Cell Viability Assay Cell Line: SW620 cells,SW620/Ad300 cells Concentration: 0.1μM,1μM,10μM,100μM Incubation Time: 72 hours Result: Decreased the resistance fold of ABCB1 substrates (Paclitaxel, Doxorubicin, Vincristine) in SW620/Ad300 cells compared to SW620 cells. 体内研究 TTT-28 (deliver orally;30mg/kg;every 3 rd day;18 days) potentiates the anticancer activity of paclitaxel due to its inhibitory effect on the efflux function of ABCB1,it enhances the inhibitory effect of paclitaxel on the growth of SW620/Ad300 tumor and promoted apoptosis. Animal Model: 5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells Dosage: 30mg/kg Administration: Deliver orally;every 3rd day;18 days Result: Lead to higher intratumoral accumulation of paclitaxel in tumors.
保存条件:-20℃