Tubulin-inhibitor-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETubulininhibitor1Cat.No.:HY-112607CASNo.:2237054-53-2分?式:C??H??N?O?分?量:368.43作?靶點(diǎn):Microtubule/Tubulin;Apoptosis作?通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥125mg/mL(339.28mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7142mL13.5711mL27.1422mL5mM0.5428mL2.7142mL5.4284mL10mM0.2714mL1.3571mL2.7142mL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備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。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，澄的儲備液可以根據(jù)儲存條件，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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(5.65mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.65mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.65mM);ClearsolutionBIOLOGICALACTIVITY?物活性Tubulininhibitor1tubulin抑制劑，靶作?于秋?仙素結(jié)合位點(diǎn)，抑制微管蛋?聚集。Tubulininhibitor1具有抗腫瘤活性，能夠?qū)е录?xì)胞G2/M期有絲分裂停滯，誘導(dǎo)細(xì)胞凋亡[1]。IC50&TargetTubulin[1]體外研究Tubulininhibitor1(Compound7a3)isatubulininhibitor,inhibitstubulinpolymerization[1].Tubulininhibitor1haspotentanti-proliferativeactivityagainstSK-OV-3,MDA-MB-231,HeLa,A549,CT26andMCF-7cells,withIC50sof16.7±3.0,31.4±0.7,32.8±2.9,67.0±0.8,58.0±2.4and35.4±5.6nM,respectively[1].Tubulininhibitor1(40,80,and160nM,48hours)markedlycausescellularmitoticarrestintheG2/Mphase,inducesapoptosisinSK-OV-3cells[1].ApoptosisAnalysis[1]CellLine:SK-OV-3cellsConcentration:40,80,and160nMIncubationTime:48hResult:InducedapoptosisinSK-OV-3cellsaftertreatmentfor48h.體內(nèi)研究Tubulininhibitor1(50mg/kg,i.p.,everytwodaysthreetimesfor20-25days)iswelltolerated,significantlyreducestumourgrowthinBalb/cnudemicebearingSK-OV-3cells[1].AnimalModel:Six-week-oldBalb/cnudemice(18-20g)beraringSK-OV-3cells[1]Dosage:50mg/kgAdministration:I.P.,everytwodaysthreetimesfor20-25daysResult:SignificantlyreducedtumourgrowthinBalb/cnudemicebearingSK-OV-3cells,withoutobviousbodyweightloss.REFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].LaiQ,etal.Design,synthesisandbiologicalevaluationofanoveltubulininhibitor7a3.EurJMedChem.2018Aug5;156:162-179.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl