Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEVincristinesulfateCat.No.:HY-N0488CASNo.:2068-78-2分?式:C??H??N?O??S分?量:923.04作?靶點(diǎn):Microtubule/Tubulin;Apoptosis作?通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:82.5mg/mL(89.38mM;Needultrasonic)掃描?維碼，H2O:50mg/mL(54.17mM;Needultrasonic)運(yùn)?溶解?案計(jì)算器獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.0834mL5.4169mL10.8338mL5mM0.2167mL1.0834mL2.1668mL10mM0.1083mL0.5417mL1.0834mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶1.請依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.75mg/mL(2.98mM);Clearsolution此?案可獲得≥2.75mg/mL(2.98mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL27.5mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)1/3www.MedChemEwww.MedChemESolubility:≥2.75mg/mL(2.98mM);Clearsolution此?案可獲得≥2.75mg/mL(2.98mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL27.5mg/mL的澄DMSO儲(chǔ)備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.75mg/mL(2.98mM);Clearsolution此?案可獲得≥2.75mg/mL(2.98mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL27.5mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性Vincristinesulfate?種抗腫瘤長花?物堿，抑制有絲分裂紡錘體中的microtubule形成，導(dǎo)致中期階段的分裂細(xì)胞停滯。它與microtubule結(jié)合的Ki為85nM。體外研究Vincristineinhibitsnetadditionoftubulindimersatassemblyendsofsteady-statemicrotubuleswithKiof85nM[1].Vincristinestabilizesthespindleapparatusresultinginfailureofthechromosomestosegregateleadingtometaphasearrestandinhibitionofmitosisatlowconcentrations.Athigherconcentrations,Vincristinemaydisruptandinducetotaldepolymerizationofmicrotubules[2].VincristineinducesapoptosisintumorcellsandinhibitsSH-SY5YcellproliferationwithIC50of0.1μM.Vincristineinducesmitoticarrestandpromotstheexpressionofcaspase-3and-9andcyclinB,whiledecreasingtheexpressionofcyclinD[3].Vincristineinducedneurotoxicityiscausedbyinterferencewithmicrotubulefunction,whichresultsinblockageofaxonaltransportandthusinaxonaldegeneration[4].體內(nèi)研究Vincristine(3mg/kg,i.p.)inducesmeangrowthdelayof>120and>52day,andrepopulatesfractionsof0.06%and5%,administratedinmicebearingbilateralsubcutaneousxenograftsRh12orRh18,respectively[5].PROTOCOLCellAssay[1]Cellsareplatedin2mLofmediumin35mmplatesataconcentrationofabout5×104cells/mLandgrowfor24hat37°Cinanatmosphereof5%CO2and95%air.Thenmediumisreplacedwithfreshmediumlackingorcontaining4nMdrugandproliferationiscontinuedfor3days.CellcountsaredoneeachdayinaCoulterCounterafterdetachingthecellswithtrypsinandEDTA.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Leukemia.2021Mar29.?CellChemBiol.2020Nov19;27(11):1359-1370.e8.?EurJMedChem.2018Feb25;146:157-170.?IntJBiolMacromol.2019Jan30;128:574-582.2/3www.MedChemEwww.MedChemE?IntJNanomedicine.2017Mar16;12:2081-2108.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Jordan,M.A.,etal.Comparisonoftheeffectsofvinblastine,vincristine,vindesine,andvinepidineonmicrotubuledynamicsandcellproliferationinvitro.CancerRes,1985.45(6):p.2741-7.[2].Gidding,C.E.,etal,Vincristinerevisited.CritRevOncolHematol,1999.29(3):p.267-87.[3].Donoso,J.A.,etal,Actionofthevincaalkaloidsvincristine,vinblastine,anddesacetylvinblastineamideonaxonalfibrillarorganellesinvitro.CancerRes,1977.37(5):p.1401-7.[4].Horton,J.K.,etal.Relationshipsbetweentumorresponsiveness,vincristinepharmacokineticsandarrestofmitosisinhumantumorxenografts.BiochemPharmacol,1988.37(20):p.3995-4000.[5].Baguley,B.C.,etal,Inhibitionofgrowthofcolon38adenocarcinomabyvinblastineandcolchicine:evidenceforavascularmechanism.EurJCancer,1991.27(4):p.482-7.[6].ZhangD,etal.Co-deliverynanoparticleswithcharacteristicsofintracellularprecisionreleasedrugsforovercomingmultidrugresistance.IntJNanomedicine.2017Mar16;12:2081-2108.McePdfHeight關(guān)注MCE中國公眾號(hào)，

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