Repotrectinib-TPX-0005-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERepotrectinibCat.No.:HY-103022CASNo.:1802220-02-5Synonyms:TPX-0005分⼦式:C₁₈H₁₈FN₅O₂分⼦量:355.37作⽤靶点:ROSKinase;TrkReceptor;Anaplasticlymphomakinase(ALK)作⽤通路:ProteinTyrosineKinase/RTK;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(70.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8140mL14.0698mL28.1397mL5mM0.5628mL2.8140mL5.6279mL10mM0.2814mL1.4070mL2.8140mL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)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.03mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.03mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Repotrectinib(TPX-0005)⼀种有效的ROS1(IC50=0.07nM)和TRK(对TRKA/B/C的IC50=0.83/0.05/0.1nM)抑制剂。Repotrectinib有效抑制WTALK(IC50=1.01nM)。Repotrectinib具有抗癌活性。IC50&TargetIC50:0.07nM(ROS1),0.83/0.05/0.1nM(TRKA/B/C),1.01nM(ALK),1.04nM(JAK2),1.66nM(LYN),5.3nM(Src),6.96nM(FAK)[1][2]体外研究Repotrectinib(TPX-0005)inhibitsmutantALKsincludingALKG1202R(IC50=1.26nM)andALKL1196M(IC50=1.08nM).Repotrectinibalsoinhibitsavarietyofotherkinases,includingJAK2,LYN,Src,andFAK(IC50=1.04,1.66,5.3,and6.96nM,respectively)[1].Repotrectinibeffectivelyovercomesthisprimaryresistance(IC50=100nMincellproliferationassay)withstronginhibitionofthephosphorylationofEML4-ALK(IC50=13nM)andtheSRCsubstratepaxillin(IC50=107nM).RepotrectinibinhibitsH2228cellmigrationinawoundhealingassaywithsimilaractivitytosaracatinib[1].体内研究Repotrectinib(TPX-0005)effectivelyinhibitstumorgrowthinvivoinALKWTandALKG1202Rxenografts[1].户使⽤本产品发表的科研⽂献•TargetOncol.2022Oct6.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DayongZhai,etal.Abstract2132:Thenovel,rationally-designed,ALK/SRCinhibitorTPX-0005overcomesmultipleacquiredresistancemechanismstocurrentALKinhibitors.CancerResearch.July2016[2].KarachaliouN,etal.CommonCo-activationofAXLandCDCP1inEGFR-mutation-positiveNon-smallcellLungCancerAssociatedWithPoorPrognosis.EBioMedicine.2018Mar;29:112-127.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica