70-09-7|2-Chloro-N1,N4-bis(4-(4,5-dihydro-1H-imidazol-2-yl)phenyl)terephthalamide|CsnPharm

CAS No.: 70-09-7

NSC-60339 Catalog No. CSN27235

NSC-60339 is an inhibitor of efflux pump and a substrate of AcrAB-TolC. It is a polybasic terephthalic acid derivative that has been studied as a potential cancer chemotherapeutic agent.

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技术信息

生物活性

描述In Gram-negative bacteria, efflux pumps are able to prevent effective cellular concentrations from being achieved for a number of antibiotics^[2]. NSC-60339, a polybasic terephthalic acid derivative, is an efflux pump inhibitor and a substrate of AcrAB-TolC, currently studied as a potential cancer chemotherapeutic agent^[3]. In WT-Pore cells, treatment with NSC-60339 resulted in an observed MIC (minimum inhibitory concentration) of 25 μM in the presence of novobiocin. Furthermore, NSC-60339 dramatically reduced the rate of efflux of a known AcrAB-TolC substrate, bisbenzamide dye H-33342 (HT), in E. coli cells^[2].
作用机制NSC-60339 binds to AcrA^[2].
参考文献

[1] Yesair DW, Kohner FA, Rogers WI, Baronowsky PE, Kensler CJ. Relationship of phthalanilide-lipid complexes to uptake and retention of 2-chloro-4',4"-di(2-imidazolin-2-yl)terephthalanilide (NSC 60339) by sensitive and resistant P388 leukemia cells. Cancer Res. 1966;26(2):202-207.
[2] Haynes KM, et al. Identification and Structure-Activity Relationships of Novel Compounds that Potentiate the Activities of Antibiotics in Escherichia coli. J Med Chem. 2017 Jul 27;60(14):6205-6219
[3] Yesair DW, et al. The retention or efflux of phthalanilide (NSC 60339)-lipid complexes by sensitive or resistant murine tumor cells and Escherichia coli B. Cancer Res. 1968 Feb;28(2):314-9

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0536 mL
- 10.2679 mL
- 20.5359 mL
- 5 mM
- 0.4107 mL
- 2.0536 mL
- 4.1072 mL
- 10 mM
- 0.2054 mL
- 1.0268 mL
- 2.0536 mL

技术信息

CAS号	70-09-7	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C26H23ClN6O2	运输	蓝冰
分子量	486.95	别名

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