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TTT-28
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TTT-28图片
CAS NO:1609138-51-3
包装:5 mg
市场价:7000元

产品介绍

产品描述

TTT-28 is a thiazole-valine peptidomimetic, and is a selective ABCB1 (P-gp/MDR1) inhibitor with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.

体外活性

In drug selected SW620/Ad300 cells, TTT-28 (0-100?μM; 72 hours) reverses ABCB1-mediated MDR and transfected HEK293/ABCB1 cells(IC50s of TTT-28 in CCD-18Co, SW620 and SW620/Ad300 cells are 213.4±11.0 μM, 89.4±3.9 μM and 92.0±5.0?μM, respectively). TTT-28 (10 μM; 2 hours) raises the ABCB1-mediated MDR and increased the accumulation of [3H]-paclitaxel in ABCB1 overexpressing cells. TTT-28 (10 μM; 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 (0-40?μM; 2 hours) interacts at the drug-substrate-binding site and actives the ATPase activity of ABCB1 in a concentration-dependent fashion.

体内活性

TTT-28 (deliver orally; 30 mg/kg; every 3 rd day; 18 days) potentiates the anticancer activity of paclitaxel due to its inhibitory effect on the efflux function of ABCB1, TTT-28 enhances the inhibitory effect of paclitaxel on the growth of SW620/Ad300 tumor and promoted apoptosis.

Cas No.

1609138-51-3

分子式

C31H31N3O6S

分子量

573.66

别名

TTT-28

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years