NLCQ-1 HCl

TargetMol
Product Code: TAR-T33699
Supplier: TargetMol
CodeSizePrice
TAR-T33699-5mg5mg£850.00
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TAR-T33699-50mg50mg£1,661.00
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TAR-T33699-100mg100mg£2,079.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
NLCQ-1 is a novel weak 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.
CAS:
221292-08-6
Formula:
C15H15Cl2N5O2
Molecular Weight:
368.22
Purity:
0.98
SMILES:
Cl.[O-][N+](=O)c1nccn1CCCNc1ccnc2cc(Cl)ccc12

References

Lunt SJ, Cawthorne C, Ali M, Telfer BA, Babur M, Smigova A, Julyan PJ, Price PM, Stratford IJ, Bloomer WD, Papadopoulou MV, Williams KJ. The hypoxia-selective cytotoxin NLCQ-1 (NSC 709257) controls metastatic disease when used as an adjuvant to radiotherapy. Br J Cancer. 2010 Jul 13;103(2):201-8. doi: 10.1038/sj.bjc.6605753. Epub 2010 Jun 29. PubMed PMID: 20588272; PubMed Central PMCID: PMC2906743. Papadopoulou MV, Bloomer WD, Torti VR, Page JG. 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. Basic Clin Pharmacol Toxicol. 2010 Jun;106(6):497-504. doi: 10.1111/j.1742-7843.2009.00530.x. Epub 2010 Jan 14. PubMed PMID: 20074267. Papadopoulou MV, Ji M, Bloomer WD. Hypoxia-dependent retinal toxicity of NLCQ-1 (NSC 709257) in BALB/c mice. Comparison with tirapazamine. Basic Clin Pharmacol Toxicol. 2011 Jun;108(6):396-9. doi: 10.1111/j.1742-7843.2010.00667.x. Epub 2011 Jan 26. PubMed PMID: 21205223. Papadopoulou MV, Bloomer WD, Torti VR, Page JG. Investigational new drug-directed toxicology and pharmacokinetic study of 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1, NSC 709257) in Beagle dogs. Basic Clin Pharmacol Toxicol. 2010 Jun;106(6):511-22. doi: 10.1111/j.1742-7843.2009.00532.x. Epub 2010 Jan 14. PubMed PMID: 20074266.