Zidovudine

Catalog No.S2579 Synonyms: Azidothymidine, NSC 602670

For research use only.

Zidovudine (ZDV, Azidothymidine, NSC 602670) 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  Chemical Structure

CAS No. 30516-87-1

Selleck's Zidovudine has been cited by 14 publications

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Biological Activity

Description Zidovudine (ZDV, Azidothymidine, NSC 602670) 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.
Targets
Reverse transcriptase [1]
In vitro

Zidovudine pretreatment has potent anti-HIV-1 activity in the newly infected T and monocytic cells but not in chronically infected cells. [1] 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. [2] Zidovudine and dideoxynucleosides deplete wild-type mitochondrial DNA levels and increase deletedmitochondrial DNA levels in cultured Kearns-Sayre syndrome fibroblasts. [3] 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. [4] 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. [5] Zidovudine could decrease the HDR efficiency. It decrease CRISPR-mediated sequence-specific genome knockin events while increases knockout efficiency[6] .

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human C8166 cells NYLHSnBpTnWwY4Tpc44h[XO|YYm= MmDERY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTJVu[W5iaX3teY5w\GWoaXPp[Y5kgSC4aYL1d{AyKGmwZnXjeIVlKGmwIHj1cYFvKEN6MU[2JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyeZMucW6mdXPl[EBkgXSxcHH0bIlkKGWoZnXjeEwhTUN3ME20[U0xPiEQvF2= NHf3R2ozOTV|NEW0NC=>
PBMC Mmm1SpVv[3Srb36gZZN{[Xl? MWGxJO69VQ>? NVTPNGlkSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDUSWtKKHKncHzpZ4F1cW:wIHnuJHBDVUNiYYSgNUB2VSxiSVO1NF0xNjByMEG0JO69VQ>? NVfQVpl2OTZ2MkCwNlc>
human H9 cells M33XR2Z2dmO2aX;uJIF{e2G7 MnvKOkBl[Xm| NHjVcVFCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJfW2jbjDpcY12dm:mZX\pZ4lmdmO7II\pdpV{KDFiM1KgbY5n\WO2ZXSgbY4hcHWvYX6gTFkh[2WubIOgbY5n\WO2ZXSge4l1cCB4LkK1JJVNKG:oII\pdpV{KHO2b3PrJIF{e2W|c3XkJIF{KGW6cILld5Nqd25ib3[gdFI1KGGwdHnn[Y4h[W[2ZYKgOkBl[Xm|IIDvd5Rqdm[nY4Tpc44h[nliRVzJV2EtKEmFNUC9NE4{KG6P MUCyNFA5PjF2OR?=
AA5 cells NYrDXYFrTnWwY4Tpc44h[XO|YYm= MXzBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDv[kBJfW2jbjDpcY12dm:mZX\pZ4lmdmO7II\pdpV{KDFiM1KgbY5n\WO2ZXSgbY4hSUF3IHPlcIx{KGmwZnXjeIVlKHerdHigNU42PiC3TDDv[kB3cXK3czDzeI9kcyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJHJmfmW{c3WgeJJidnOlcnnweIF{\SCkeTDbN2heXFSSIHnuZ49zeG:{YYTpc44h[XO|YYmsJGlEPTB;MD6zJI5O M37aSVIxODh4MUS5
CEM cells M2HFWGZ2dmO2aX;uJIF{e2G7 MY\Dc45k\W62cnH0bY9vKG:oIITo[UBlenWpIILld5VtfGmwZzDpckA2OCVicnXkeYN1cW:wIH;mJJRp\SC4aYLhcEBkgXSxcHH0bIlkKGWoZnXjeEBi\2GrboP0JGhKXi1zIILldIxq[2G2aX;uJIlvKEOHTTDj[YxteyxiRVO1NF0xNjN{IH7N NVfESYVLOjF3M{KwOi=>
MT4 cells NXPRTppDTnWwY4Tpc44h[XO|YYm= M2LJR|Qh\GG7cx?= NGHwPIVCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIEPCJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolzfXNvaX7keYNm\CCleYTvdIF1cG:pZX7pZ4l1gSCrbjDNWFQh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IF3UWEBie3OjeTygSWM2OD1yLkegcm0> NXLCOotzOTd7NkS3PVY>
human MT2 cells M3TuZ2Z2dmO2aX;uJIF{e2G7 MnfWNUBp MnH5RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSC|dXL0fZBmKEJvM1KgbY5n\WO2ZXSgbY4hOSCqcj3wdoV1emWjdHXkJIh2dWGwIF3UNkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIH31cJRq[3mlbHWgdoVxdGmlYYTpc44hdWWjc4Xy[YQhd25iZHH5JFUheG:|dHnu[oVkfGmxbjDifUBTXCCVUFGsJGVEPTB;MT6yJI5O NEfwTm0yQDNzNkWyNS=>
C8166 cells M2Lqb2Z2dmO2aX;uJIF{e2G7 M{f6[WlvcGmkaYTpc44hd2ZiSFnWNU0{SiC{ZYDsbYNifGmxbjDpckBEQDF4NjDj[YxteyxiRVO1NF0yNjlibl2= NHnGcnEyPjJ5OUe3Ny=>
CEM-SS cell M{fFdmZ2dmO2aX;uJIF{e2G7 NX64UVAyUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KHSqZTDITXYuOS2rbnT1Z4VlKGO7dH;wZZRpcWNiZX\m[YN1KGmwIFPFUU1UWyClZXzsJIxqdmVuIFnDOVA:OC5yMEKg{txO MoXvO|Y2ODZ5OB?=
PBLs NVr0[HVoTnWwY4Tpc44h[XO|YYm= M2TTOGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JJN2[nS7cHWgbZNwdGG2ZTDHJJN1emGrbjDpckBRSky|IDjw[ZJqeGincnHsJIJtd2:mIHz5cZBpd2O7dHXzLUwhUUN3ME2wMlAxOiEQvF2= MmHONVE4ODh7MUO=
human lymphocyte CEM/0 cell line NXXqWmRnTnWwY4Tpc44h[XO|YYm= M13MWGFvfGliSFnWMVEh[WO2aY\peJkhcW5iaIXtZY4hdHmvcHjvZ5l1\SCFRV2vNEBk\WyuIHzpcoUtKEWFNUC9NE4xODNizszN Mn:xPFQ4QDlyNB?=
Jurkat cell MoD0SpVv[3Srb36gZZN{[Xl? MoPBTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiSFnWMVEhcW6oZXP0[YQhUnW{a3H0JINmdGxibHnu[ZMtKEmFNUC9NE4xOSEQvF2= NVLkTXlpPzh|N{KyNC=>
human H9 cells M4Xv[WN6fG:2b4jpZ4l1gSCjc4PhfS=> MoDyOkBl[Xm| MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIPUBk\WyuczDh[pRmeiB4IHThfZMh[nliTWTUJIF{e2G7LDDFR|UxRTBwMEGg{txO MXeyNFg1Pjh4OB?=
C3H/3T3 cells NXPwSHZ3TnWwY4Tpc44h[XO|YYm= NWrzeJRZS2:wY3XueJJifGmxbjDv[kBkd22yb4Xu[EBz\XG3aYLl[EB1dyCrbnjpZol1KEiLVj2xJIlv\HWlZXSgZ5l1d3CjdHjv[4VvcWOrdImgc4YhVVOYLXnu[JVk\WRidILhcpNnd3KvYYTpc44hd2ZiQ{PIM|NVOyClZXzsd{BjgSB3MDWsJGVEPTB;MD6wNkDPxE1? MVWyNFE3PzF6
U937 cells NIP2UppHfW6ldHnvckBie3OjeR?= M3XydGVn\mWldHn2[UBkd26lZX70doF1cW:wIILldZVqemWmIH\vdkBidnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBO[WO{b4DoZYdmKGOnbHygcIlv\SCxZjDVPVM4KGOnbHzzJI9nKEi3bXHuJIJ6KFiWVDDhd5NigSxiRVO1NF0xNjB|IN88US=> Moi0O|k{OjV{Nh?=

Protocol (from reference)

Solubility (25°C)

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.

Chemical Information

Molecular Weight 267.24
Formula

C10H13N5O4

CAS No. 30516-87-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-]

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01818258 Completed Drug: ZDV+3TC+LPV/r HIV Positive|Malnourished International Maternal Pediatric Adolescent AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institute of Mental Health (NIMH) October 26 2015 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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Frequently Asked Questions

Question 1:
Do you happen to have any information regarding the half-life of AZT?

Answer:
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.

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