NSC-60339 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

486.95

C₂₆H₂₃ClN₆O₂

70-09-7

Solid

Off-white to light yellow

O=C(C1=CC=C(C=C1Cl)C(NC2=CC=C(C=C2)C3=NCCN3)=O)NC4=CC=C(C=C4)C5=NCCN5

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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 19

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]