Repotrectinib-TPX-0005-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERepotrectinibCat.No.:HY-103022CASNo.:1802220-02-5Synonyms:TPX-0005分?式:C??H??FN?O?分?量:355.37作?靶點:ROSKinase;TrkReceptor;Anaplasticlymphomakinase(ALK)作?通路:ProteinTyrosineKinase/RTK;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(70.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8140mL14.0698mL28.1397mL5mM0.5628mL2.8140mL5.6279mL10mM0.2814mL1.4070mL2.8140mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.03mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.03mM);ClearsolutionBIOLOGICALACTIVITY?物活性Repotrectinib(TPX-0005)?種有效的ROS1(IC50=0.07nM)和TRK(對TRKA/B/C的IC50=0.83/0.05/0.1nM)抑制劑。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]體外研究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].體內(nèi)研究Repotrectinib(TPX-0005)effectivelyinhibitstumorgrowthinvivoinALKWTandALKG1202Rxenografts[1].戶使?本產(chǎn)品發(fā)表的科研?獻?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