Tubulin-inhibitor-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETubulininhibitor1Cat.No.:HY-112607CASNo.:2237054-53-2分⼦式:C₂₁H₂₄N₂O₄分⼦量:368.43作⽤靶点:Microtubule/Tubulin;Apoptosis作⽤通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥125mg/mL(339.28mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7142mL13.5711mL27.1422mL5mM0.5428mL2.7142mL5.4284mL10mM0.2714mL1.3571mL2.7142mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.65mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.65mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.65mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Tubulininhibitor1tubulin抑制剂，靶作⽤于秋⽔仙素结合位点，抑制微管蛋⽩聚集。Tubulininhibitor1具有抗肿瘤活性，能够导致细胞G2/M期有丝分裂停滞，诱导细胞凋亡[1]。IC50&TargetTubulin[1]体外研究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.体内研究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—您⾝边的抑制剂⼤师www.MedChemE[1].LaiQ,etal.Design,synthesisandbiologicalevaluationofanoveltubulininhibitor7a3.EurJMedChem.2018Aug5;156:162-179.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl