BO-264-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEBO-264Cat.No.:HY-135960CASNo.:2408648-20-2分⼦式:C₁₈H₁₉N₅O₃分⼦量:353.38作⽤靶点:FGFR;Apoptosis作⽤通路:ProteinTyrosineKinase/RTK;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(141.49mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8298mL14.1491mL28.2981mL5mM0.5660mL2.8298mL5.6596mL10mM0.2830mL1.4149mL2.8298mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.89mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.89mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.89mM);Clearsolution1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性BO-264⼀种⾼效，⼝服活性的转化酸性卷曲螺旋3(TACC3)抑制剂，IC50为188nM，Kd为1.5nM。BO-264特异性阻断FGFR3-TACC3融合蛋⽩的功能。BO-264诱导纺锤体检查点依赖的有丝分裂阻滞，DNA损伤和细胞凋亡(apoptosis)。BO-264具有⼴谱抗肿瘤活性。IC50&TargetIC50:188nM(Transformingacidiccoiled-coil3(TACC3))[1]Kd:1.5nM(TACC3)[1]体外研究BO-264(500nM;48hours;JIMT-1cells)treatmentinducesaprominentincrease(from4.1%to45.6%)inthefractionofapoptoticcellsasassessedbyAnnexinV/PIstaining[1].BO-264(500nM;24hours;RT112cells)treatmentdecreasesERK1/2phosphorylation,whichisamarkerforactivatedFGFRsignalingalongwithastrongmitoticarrest[1].BO-264inhibitscellviabilitywithIC50valuesof190nM,160nM,120nM,130nMand360nMforJIMT-1,HCC1954,MDA-MB-231,MDA-MB-436andCAL51,respectively.BO-264specificallytargetsbreastcancercellswhilesparingnormalcells.BO-264treatmentsignificantlyreducestheaveragecolonynumberofJIMT-1cells[1].BO-264inhibitstheviabilityofcancercellswithFGFR3-TACC3fusionwithIC50valuesof0.3μMand3.66μMforRT112andRT4,respectively[1].BO-264exhibitsaremarkableanti-canceractivityagainstmorethan90%oftheNCI26760humancancercelllinesrepresentingninedifferentsubpanelswithGI50valueslessthan1μM[1].BO-264inducesmitoticarrest(prominentinducesp-HistoneH3(Ser10)),apoptosis(cleavedPARP)andDNAdamage,causesaberrantspindleformationandreducescentrosomallocalizationofTACC3inJIMT-1cells[1].ApoptosisAnalysis[1]CellLine:JIMT-1cellsConcentration:500nMIncubationTime:48hoursResult:Inducedaprominentincrease(from4.1%to45.6%)inthefractionofapoptoticcellsasassessedbyAnnexinV/PIstaining.WesternBlotAnalysis[1]CellLine:RT112cellsConcentration:500nMIncubationTime:24hoursResult:DecreasedERK1/2phosphorylation.2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究BO-264(25mg/kg;oraladministration;daily;for3-4weeks;femalenudemice)treatmentshowsasignificantsuppressionoftumorgrowth.BO-264iswelltoleratedsincetreatmentdoesnotcausesasignificantbodyweightlossandorgantoxicity[1].AnimalModel:FemalenudemiceinjectedwithJIMT-1cells[1]Dosage:25mg/kgAdministration:Oraladministration;daily;for3-4weeksResult:Showedasignificantsuppressionoftumorgrowth.REFERENCES[1].AkbulutO,etal.AHighlyPotentTACC3InhibitorasaNovelAnti-cancerDrugCandidate.MolCancerTher.2020Mar26.pii:molcanther.0957.2019.McePdfHeightCaution:Producth