Zidovudine

Catalog No.S2579 Synonyms: Azidothymidine, NSC 602670,Retrovir

For research use only.

Zidovudine (ZDV, Azidothymidine, NSC 602670,Retrovir) 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 15 publications

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Biological Activity

Description Zidovudine (ZDV, Azidothymidine, NSC 602670,Retrovir) 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 MXfGeY5kfGmxbjDhd5NigQ>? NIH4WWdCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJfW2jbjDpcY12dm:mZX\pZ4lmdmO7II\pdpV{KDFiaX7m[YN1\WRiaX6gbJVu[W5iQ{ixOlYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJ2ey2rbnT1Z4VlKGO7dH;wZZRpcWNiZX\m[YN1NCCHQ{WwQVRmNTB4IN88US=> NVXRcXpuOjF3M{S1OFA>
PBMC MUTGeY5kfGmxbjDhd5NigQ>? MnuzNUDPxE1? M4nibmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiVFXLTUBz\XCuaXPheIlwdiCrbjDQRm1EKGG2IEGgeW0tKEmFNUC9NE4xODBzNDFOwG0> MWKxOlQzODB{Nx?=
human H9 cells Mne0SpVv[3Srb36gZZN{[Xl? NGjk[Fc3KGSjeYO= MnXQRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTJVu[W5iaX3teY5w\GWoaXPp[Y5kgSC4aYL1d{AyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIFi5JINmdGy|IHnu[oVkfGWmIIfpeIghPi5{NTD1UEBw\iC4aYL1d{B{fG:lazDhd5Nme3OnZDDhd{BmgHC{ZYPzbY9vKG:oIICyOEBidnSrZ3XuJIFnfGW{IE[g[IF6eyCyb4P0bY5n\WO2aX;uJIJ6KEWOSWPBMEBKSzVyPUCuN{BvVQ>? Mm\ONlAxQDZzNEm=
AA5 cells M{X2SWZ2dmO2aX;uJIF{e2G7 M2TWUWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JI9nKEi3bXHuJIludXWwb3Tl[olkcWWwY4mgeolzfXNiMTCzRkBqdm[nY4Tl[EBqdiCDQUWgZ4VtdHNiaX7m[YN1\WRid3n0bEAyNjV4IIXMJI9nKH[rcoXzJJN1d2OtIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhWmW4ZYLz[UB1emGwc3PybZB1[XOnIHL5JHs{UF2WVGCgbY5kd3Kyb4LheIlwdiCjc4PhfUwhUUN3ME2wMlMhdk1? MmntNlAxQDZzNEm=
CEM cells NVLocVM6TnWwY4Tpc44h[XO|YYm= NYfx[5pTS2:wY3XueJJifGmxbjDv[kB1cGViZIL1[{Bz\XO3bITpcochcW5iNUClJJJm\HWldHnvckBw\iC2aHWgeolz[WxiY4n0c5BifGirYzDl[oZm[3RiYXfhbY5{fCCKSW[tNUBz\XCuaXPheIlwdiCrbjDDSW0h[2WubIOsJGVEPTB;MD6zNkBvVQ>? M4DT[lIyPTN{ME[=
MT4 cells NX76bIZQTnWwY4Tpc44h[XO|YYm= NUWxSIJyPCCmYYnz NXL1dXZFSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqenW|LXnu[JVk\WRiY4n0c5BifGixZ3XubYNqfHliaX6gUXQ1KGOnbHzzJIFnfGW{IESg[IF6eyCkeTDNWHQh[XO|YYmsJGVEPTB;MD63JI5O MnnyNVc6PjR5OU[=
human MT2 cells NVfFV4NjTnWwY4Tpc44h[XO|YYm= MXSxJIg> M3H5XGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFic4XieJlx\SCELUPCJIlv\mWldHXkJIlvKDFiaIKtdJJmfHKnYYTl[EBpfW2jbjDNWFIh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDteYx1cWO7Y3zlJJJmeGyrY3H0bY9vKG2nYYP1doVlKG:wIHThfUA2KHCxc4TpcoZm[3Srb36gZpkhWlRiU2DBMEBGSzVyPUGuNkBvVQ>? NH7Oe3EyQDNzNkWyNS=>
C8166 cells MV7GeY5kfGmxbjDhd5NigQ>? NHf3b5pKdmirYnn0bY9vKG:oIFjJWlEuO0JicnXwcIlk[XSrb36gbY4hSzhzNk[gZ4VtdHNuIFXDOVA:OS57IH7N NUnkUGh6OTZ{N{m3O|M>
CEM-SS cell MUHGeY5kfGmxbjDhd5NigQ>? NFXldpVKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhfGinIFjJWk0yNWmwZIXj[YQh[3m2b4DheIhq[yCnZn\lZ5QhcW5iQ1XNMXNUKGOnbHygcIlv\SxiSVO1NF0xNjByMjFOwG0> Mn;MO|Y2ODZ5OB?=
PBLs NUTYfWJoTnWwY4Tpc44h[XO|YYm= NXXWV2wySW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5Qhe3WkdInw[UBqe2:uYYTlJGche3S{YXnuJIlvKFCETIOgLJBmemmyaHXyZYwh[myxb3SgcJlueGixY4n0[ZMqNCCLQ{WwQVAvODB{IN88US=> M3PPZ|EyPzB6OUGz
human lymphocyte CEM/0 cell line M3\1O2Z2dmO2aX;uJIF{e2G7 MlXzRY51cSCKSW[tNUBi[3Srdnn0fUBqdiCqdX3hckBtgW2yaH;jfZRmKEOHTT:wJINmdGxibHnu[UwhTUN3ME2wMlAxOyEQvF2= NILNRmI5PDd6OUC0
Jurkat cell NXzZSIxoTnWwY4Tpc44h[XO|YYm= MXXJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCKSW[tNUBqdm[nY4Tl[EBLfXKtYYSgZ4VtdCCuaX7ld{whUUN3ME2wMlAyKM7:TR?= NFHBT|E4QDN5MkKw
human H9 cells NEXwNppEgXSxdH;4bYNqfHliYYPzZZk> Ml\5OkBl[Xm| NXHjcpZ{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUDliY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JG1VXCCjc4PhfUwhTUN3ME2wMlAyKM7:TR?= NHr5cZczODh2Nki2PC=>
C3H/3T3 cells NYO5ToRoTnWwY4Tpc44h[XO|YYm= NGqzdYdEd26lZX70doF1cW:wIH;mJINwdXCxdX7kJJJmeXWrcnXkJJRwKGmwaHnibZQhUEmYLUGgbY5lfWOnZDDjfZRweGG2aH;n[Y5q[2m2eTDv[kBOW1ZvaX7keYNm\CC2cnHud4Zwem2jdHnvckBw\iCFM1ivN3Q{KGOnbHzzJIJ6KDVyJTygSWM2OD1yLkCyJO69VQ>? M{j6NFIxOTZ5MUi=
U937 cells NX;yc2s3TnWwY4Tpc44h[XO|YYm= M3j3TmVn\mWldHn2[UBkd26lZX70doF1cW:wIILldZVqemWmIH\vdkBidnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBO[WO{b4DoZYdmKGOnbHygcIlv\SCxZjDVPVM4KGOnbHzzJI9nKEi3bXHuJIJ6KFiWVDDhd5NigSxiRVO1NF0xNjB|IN88US=> M{jIUVc6OzJ3Mk[=

Protocol (from reference)

Solubility (25°C)

In vitro

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)

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03991013 Completed Drug: Dolutegravir 50 mg|Drug: Placebo HIV Infections University of Cape Town|Wellcome Trust|Médecins Sans Frontières Belgium August 8 2019 Phase 2
NCT03642704 Completed Drug: Reinforced preventive ARV therapy Mother to Child HIV Transmission ANRS Emerging Infectious Diseases February 22 2017 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-11-29)

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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