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Zidovudine Reverse Transcriptase Remmer

Cat.nr.: S2579

Zidovudine (ZDV, Azidothymidine, NSC 602670) is een nucleoside-analoog reverse transcriptase-remmer, gebruikt voor de behandeling van HIV. Deze verbinding zou de HDR-efficiëntie kunnen verlagen en CRISPR-gemedieerde sequentie-specifieke gen-knockin-gebeurtenissen kunnen verminderen, terwijl de knock-out-efficiëntie toeneemt.
Zidovudine  Reverse Transcriptase Remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 267.24

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.90%
99.90

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving PMID
human C8166 cells Function assay Antiviral activity against Human immunodeficiency virus 1 infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect, EC50=4e-06 μM
PBMC Function assay 1 μM Antiviral activity against HIV1 TEKI replication in PBMC at 1 uM, IC50=0.00014 μM
human H9 cells Function assay 6 days Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.3 nM
AA5 cells Function assay Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.3 nM
CEM cells Function assay Concentration of the drug resulting in 50% reduction of the viral cytopathic effect against HIV-1 replication in CEM cells, EC50=0.32 nM
MT4 cells Function assay 4 days Antiviral activity against HIV1 3B assessed as inhibition of virus-induced cytopathogenicity in MT4 cells after 4 days by MTT assay, EC50=0.7 nM
human MT2 cells Function assay 1 h Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=1.2 nM
C8166 cells Function assay Inhibition of HIV1-3B replication in C8166 cells, EC50=1.9 nM
CEM-SS cell Function assay Inhibitory activity against the HIV-1-induced cytopathic effect in CEM-SS cell line, IC50=0.002 μM
PBLs Function assay Antiviral activity against subtype isolate G strain in PBLs (peripheral blood lymphocytes), IC50=0.002 μM
human lymphocyte CEM/0 cell line Function assay Anti HIV-1 activity in human lymphocyte CEM/0 cell line, EC50=0.003 μM
Jurkat cell Function assay Inhibitory concentration against HIV-1 infected Jurkat cell lines, IC50=0.01 μM
human H9 cells Cytotoxicity assay 6 days Cytotoxicity against human H9 cells after 6 days by MTT assay, EC50=0.01 μM
C3H/3T3 cells Function assay Concentration of compound required to inhibit HIV-1 induced cytopathogenicity of MSV-induced transformation of C3H/3T3 cells by 50%, EC50=0.02 μM
U937 cells Function assay Effective concentration required for antiviral activity against Macrophage cell line of U937 cells of Human by XTT assay, EC50=0.03 μM
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht 267.24 Formule

C10H13N5O4

Opslag (vanaf de datum van ontvangst)
CAS-nr. 30516-87-1 SDF downloaden Opslag van stamoplossingen

Synoniemen Azidothymidine, NSC 602670 Smiles CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-]

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 53 mg/mL (198.32 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 53 mg/mL

Water : 26 mg/mL

Molariteitscalculator

Massa Concentratie Volume Molecuulgewicht
Verdunningscalculator Molecuulgewichtcalculator

In vivo
Batch:

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC50/Ki
Reverse transcriptase
In vitro

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 this compound decreases p24 antigen levels modestly, decreased HIV-1 gag by 19-fold, and inhibits detection of 2-LTR HIV-1 DNA. This compound and dideoxynucleosides deplete wild-type mitochondrial DNA levels and increase deletedmitochondrial DNA levels in cultured Kearns-Sayre syndrome fibroblasts. This chemical (AZT, 0.1-50 mM) has a concentration dependent suppressive effect on the growth of granulocyte-monocyte colony forming unit (CFU-GM) derived colonies. This compound exposure also induces a concentration dependent suppressive effect (35-90%) on GM-CSF receptor type alpha (GM-CSFR alpha) gene expression. It 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. This chemical 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. It also inhibits protein kinase C (PKC) activity in a concentration- and time-dependent manner, causing 50% inhibition at 10 mM within 3 hours. This compound-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. This compound could decrease the HDR efficiency. It decrease CRISPR-mediated sequence-specific genome knockin events while increases knockout efficiency .

Referenties
  • [4] https://pubmed.ncbi.nlm.nih.gov/12084393/
  • [5] https://pubmed.ncbi.nlm.nih.gov/7646543/
  • [6] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4461869/

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2026-08-25)

NCT-nummer Werving Aandoeningen Sponsor/medewerkers Startdatum Fasen
NCT01419561 RECRUITING
KSHV Inflammatory Cytokine Syndrome (KICS); KSHV; HHV-8
National Cancer Institute (NCI)
2011-09-08 PHASE2
NCT00092222 ACTIVE_NOT_RECRUITING
Lymphoproliferative Disorder; HHV-8; Malignancy; HIV
National Cancer Institute (NCI)
2004-10-28 PHASE2
NCT02737046 COMPLETED
Adult T-cell Leukemia-Lymphoma; ATLL
University of Miami
2016-12-12 PHASE2
NCT04731103 COMPLETED
Aicardi-Goutières Syndrome
University of Edinburgh
2022-08-24 PHASE2
NCT00799864 COMPLETED
HIV-1
Janssen Sciences Ireland UC
2011-01 PHASE2
NCT03088410 COMPLETED
HIV; Insulin Sensitivity; Diabetes Mellitus
Ann & Robert H Lurie Children's Hospital of Chicago
2016-08-22 PHASE4

Veelgestelde vragen (Frequently Asked Questions)

Vraag 1:
Do you happen to have any information regarding its half-life?

Antwoord:
Its half-life in human is available (http://www.rxlist.com/retrovir-drug/clinical-pharmacology.htm), about 0.5-3 hours in adult subjects.