NSC-60339 |
Catalog No.GC60273 |
NSC-60339, un inhibidor de la bomba de expulsiÓn y un sustrato de AcrAB-TolC, es un derivado del Ácido tereftÁlico polibÁsico estudiado como agente quimioterapéutico potencial contra el cÁncer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1970/9/7
Sample solution is provided at 25 µL, 10mM.
NSC-60339, an efflux pump inhibitor and a substrate of AcrAB-TolC, is a polybasic terephthalic acid derivative studied as a potential cancer chemotherapeutic agent[1][2].
NSC 60339 has been correlated with the sensitivity, resistance, or cross-resistance of 7 tumor lines to phthalanilide treatment in vivo. The sensitive tumors (L1210, L1210/MTX, L1210/ara-C, and P815) rapidly takes up the drug and retained it primarily as lipid-bound drug for the 24-hr experimental period. The resistant tumor, L1210/NSC 60339, and 2 cross-resistant tumors, P388/VCR and P815/VLB, took up as much drug as the sensitive tumors did by 0.5 hr, but there was an efflux of lipid-bound drug from these resistant tumors by 24 hr[3].
[1]. D. W. Yesair, et al. 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 RESEARCH 26 Part 1: 202-207, February 1966. [2]. 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. [3]. 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. [4]. Abdali N, et al. Reviving Antibiotics: Efflux Pump Inhibitors That Interact with AcrA, a Membrane Fusion Protein of the AcrAB-TolC Multidrug Efflux Pump. ACS Infect Dis. 2017 Jan 13;3(1):89-98.
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