NLCQ-1 - CAS 221292-08-6
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Not Intended for Therapeutic Use. For research use only.
NLCQ-1 is a novel weakly DNA-intercalative bioreductive compound. NLCQ-1 exhibited a C50 of 44 microM. NLCQ-1 demonstrated significant hypoxic selectivity in several rodent (V79, EMT6, SCCVII) or human (A549, OVCAR-3) tumor cell lines. Its potency as a hypoxic cytotoxin ranged between 10 and 136 microM x h, for the cell lines tested, at 30 microM input concentration. NLCQ-1 was a very potent and efficient radiosensitizer of hypoxic V79 cells, providing SER values of 2.27-2.56 at 20-80 microM concentration (measured at 10% survival level). Preclinical results suggest a possible use of NLCQ-1 as adjuvants to radiotherapy.
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NLCQ-1; NSC 709257
Current Developer:
Northwestern University.
1.Advantage of combining NLCQ-1 (NSC 709257) with radiation in treatment of human head and neck xenografts.
Papadopoulou MV1, Bloomer WD, Taylor AP, Hernandez M, Blumenthal RD, Hollingshead MG. Radiat Res. 2007 Jul;168(1):65-71.
NLCQ-1 (NSC 709257), a hypoxia-selective cytotoxin that targets DNA through weak intercalation, was investigated for efficacy in combination with single or fractionated radiotherapy of human head and neck xenografts. A staged tumor experiment was performed in tumor-bearing female athymic nude mice that were locally irradiated with or without NLCQ-1. Tumor hypoxia was assessed by immunohistochemistry for pimonidazole adducts in tumors of varying weight. Fractionated radiation, depending on the dose, was administered either once daily for 4 days or once daily for 4 days followed by a 7-day rest and repeat. NLCQ-1 was administered i.p. at 15 mg/kg alone or 45 min before each radiation dose. Hypoxia (1-52%) was detected in all tumors and was positively correlated with tumor size. NLCQ-1 alone resulted in about 10 days of tumor growth delay, measured at sixfold the tumor's original size, without causing toxicity. All combination treatments with NLCQ-1 were more effective than treatments with radiation alone.
2.Investigational new drug-directed, 5-day repeat dose toxicity study of 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1, NSC 709257) administered with or without Taxol in Sprague-Dawley rats.
Papadopoulou MV1, Bloomer WD, Torti VR, Page JG. Basic Clin Pharmacol Toxicol. 2010 Jun;106(6):497-504. doi: 10.1111/j.1742-7843.2009.00530.x. Epub 2010 Jan 14.
In pre-clinical studies, 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1, NSC 709257) is a weak DNA-intercalating, hypoxia-selective cytotoxin with a promising profile as an adjuvant to radio/chemotherapy and it is about to enter phase I clinical trials. The present investigation was undertaken to further evaluate potential systemic toxicity induced by i.v. doses of NLCQ-1 alone or in combination with Taxol in Sprague-Dawley rats, in support of an investigational new drug application. Doses of NLCQ-1 were based on previous range-finding studies. In the present study, NLCQ-1 was administered either alone, at 0, 6, 9 or 12 mg/kg/dose to male rats and 8, 12 or 16 mg/kg/dose to female rats or, at 9 (male rats) and 12 (female rats) mg/kg/dose, in combination with Taxol, on a qd x 5 schedule. Taxol was administered i.v. at 3.5 mg/kg/dose 1 hr before NLCQ-1. Observations were recorded for mortality/moribundity, clinical signs of toxicity, body weights, food consumption, haematology, clinical chemistry, gross lesions at necropsy and histopathology.
3.The hypoxia-selective cytotoxin NLCQ-1 (NSC 709257) controls metastatic disease when used as an adjuvant to radiotherapy.
Lunt SJ1, Cawthorne C, Ali M, Telfer BA, Babur M, Smigova A, Julyan PJ, Price PM, Stratford IJ, Bloomer WD, Papadopoulou MV, Williams KJ. Br J Cancer. 2010 Jul 13;103(2):201-8. doi: 10.1038/sj.bjc.6605753. Epub 2010 Jun 29.
BACKGROUND: Metastases cause most cancer-related deaths. We investigated the use of hypoxia-selective cytotoxins as adjuvants to radiotherapy in the control of metastatic tumour growth.
4.Potentiation of alkylating agents by NLCQ-1 or TPZ in vitro and in vivo.
Papadopoulou MV1, Ji X, Bloomer WD. J Exp Ther Oncol. 2006;5(4):261-72.
PURPOSE: To investigate potential synergistic interactions between bioreductive agents, either NLCQ-1 or tirapazamine (TPZ) and two alkylating chemotherapeutic drugs, and how such interactions compare in vitro and in vivo.
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CAS 221292-08-6 NLCQ-1

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