中文名称: | TTT-28 | ||||
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英文名称: | TTT-28 | ||||
别名: | TTT-28 TTT-28 | ||||
CAS No: | 1609138-51-3 | 分子式: | C31H31N3O6S | 分子量: | 573.66 |
CAS No: | 1609138-51-3 | ||||
分子式: | C31H31N3O6S | ||||
分子量: | 573.66 |
基本信息
产品编号: |
T11028 |
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产品名称: |
TTT-28 |
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CAS: |
1609138-51-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
二年 |
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分子量: |
573.66 |
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化学名: |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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)。 |
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靶点 |
P-glycoprotein |
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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 |
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Cell Line: |
SW620 cells,SW620/Ad300 cells |
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Concentration: |
0.1μM,1μM,10μM,100μM |
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Incubation Time: |
72 hours |
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Result: |
Decreased the resistance fold of ABCB1 substrates (Paclitaxel, Doxorubicin, Vincristine) in SW620/Ad300 cells compared to SW620 cells. |
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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. |
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Animal Model: |
5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells |
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Dosage: |
30mg/kg |
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Administration: |
Deliver orally;every 3rd day;18 days |
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Result: |
Lead to higher intratumoral accumulation of paclitaxel in tumors. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )