Catalog No.S2579 Synonyms: Azidothymidine, NSC 602670
Molecular Weight(MW): 267.24
Zidovudine (ZDV) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV. It could decrease the HDR efficiency and decrease CRISPR-mediated sequence-specific genome knockin events while increaseing knockout efficiency.
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Choose Selective Reverse Transcriptase Inhibitors
|Description||Zidovudine (ZDV) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV. It could decrease the HDR efficiency and decrease CRISPR-mediated sequence-specific genome knockin events while increaseing knockout efficiency.|
Zidovudine pretreatment has potent anti-HIV-1 activity in the newly infected T and monocytic cells but not in chronically infected cells.  Inhibition of reverse transcription by Zidovudine decreases p24 antigen levels modestly, decreased HIV-1 gag by 19-fold, and inhibits detection of 2-LTR HIV-1 DNA.  Zidovudine and dideoxynucleosides deplete wild-type mitochondrial DNA levels and increase deletedmitochondrial DNA levels in cultured Kearns-Sayre syndrome fibroblasts.  Zidovudine (AZT, 0.1-50 mM) has a concentration dependent suppressive effect on the growth of granulocyte-monocyte colony forming unit (CFU-GM) derived colonies. Zidovudine exposure also induces a concentration dependent suppressive effect (35-90%) on GM-CSF receptor type alpha (GM-CSFR alpha) gene expression. Zidovudine causes a much lower decrease (15-22%) on the IL-3 receptor type alpha (IL-3R alpha) message level, and has an insignificant effect on glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and c-myc message levels.  Zidovudine causes a concentration-dependent inhibition in the levels of the mRNA of Epo receptors and c-fos, whereas the level of c-myc mRNA is unaffected. Zidovudine also inhibits protein kinase C (PKC) activity in a concentration- and time-dependent manner, causing 50% inhibition at 10 mM within 3 hours. Zidovudine-induced down-regulation of Epo receptors and c-fos expression coupled with inhibition of Epo receptor-mediated signal transduction through PKC are significant contributory factors to AZT-induced erythroid toxicity.  Zidovudine could decrease the HDR efficiency. It decrease CRISPR-mediated sequence-specific genome knockin events while increases knockout efficiency .
-  Chiang G, et al. Clin Ther,?996, 18(6), 1080-1092.
-  Panther LA, et al. J Med Virol,?999, 58(2), 165-173.
-  Wang H, et al. Biochim Biophys Acta,?996, 1316(1), 51-59.
|In vitro||DMSO||53 mg/mL (198.32 mM)|
|Water||53 mg/mL warmed (198.32 mM)|
|Ethanol||18 mg/mL warmed (67.35 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||Azidothymidine, NSC 602670|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01441063||Recruiting||Castleman Disease|Castlemans Disease|Giant Lymph Node Hyperplasia||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||August 6, 2011||Phase 2|
|NCT00001644||Completed||HIV Infection||National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC)||March 3, 1997||Phase 1|
|NCT02437110||Enrolling by invitation||Amyotrophic Lateral Sclerosis||National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC)||April 23, 2015||Phase 1|
|NCT02737046||Recruiting||Adult T-cell Leukemia-Lymphoma|ATLL||University of Miami||November 2016||Phase 2|
|NCT02832778||Recruiting||HIV||St Stephens Aids Trust|Mylan Inc.|United States Agency for International Development (USAID)||September 2016||Phase 1|
|NCT02712801||Recruiting||HIV/AIDS and Infections||National Center for Women and Childrens Health, China CDC|National Center for AIDS/STD Control and Prevention, China CDC|Maternal and Child Health Hospital of Yunan Province|Maternal and Child Health Hospital of Sichuan Province|Maternal and Child Health Hospital of Guangxi Province|Maternal and Child Health Hospital of Xinjiang Uygur Autonomous Region|Guangdong Provincial Maternal and Child Health Hospital||April 2016||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Do you happen to have any information regarding the half-life of AZT？
The Half-life of S2579 in human is available (http://www.rxlist.com/retrovir-drug/clinical-pharmacology.htm), about 0.5-3 hours in adult subjects.