Luxeptinib-CG-806-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELuxeptinibCat.No.:HY-139535CASNo.:1616428-23-9Synonyms:CG-806分?式:C??H??F?N?O?分?量:495.43作?靶點(diǎn):FLT3;Btk作?通路:ProteinTyrosineKinase/RTK儲(chǔ)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(252.31mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0184mL10.0922mL20.1845mL5mM0.4037mL2.0184mL4.0369mL10mM0.2018mL1.0092mL2.0184mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.20mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.20mM);ClearsolutionBIOLOGICALACTIVITY?物活性Luxeptinib(CG-806)?種具有?服活性、可逆的、?流的?共價(jià)的有效pan-FLT3/pan-BTK抑制劑。Luxeptinib誘導(dǎo)急性髓系??病細(xì)胞周期阻滯、凋亡或?噬[1][2][3][4]。IC50&TargetPan-FLT3/Pan-BTK[1]體外研究Luxeptinib(MEC-1CLLcells;0.1~10μM;72hours)inhibitscellsproliferationwithanIC50of32nM[1].LuxeptinibinhibitsBCRsignaling-inducedphosphorylationofBTK,PLCg2,AKT,ERK1/2,S6ribosomalproteinandstronglysuppressesSYKphosphorylationinprimarychroniclymphocyticleukemia(CLL)cells[1].Luxeptinib(MV4-11cells;500pM;1hour)completelyinhibitsphosphorylationofFLT3andSTAT5[2].CellProliferationAssay[1]CellLine:MEC-1CLLcellsConcentration:0.1~10μMIncubationTime:72hoursResult:InhibitedcellsproliferationwithanIC50of32nM.REFERENCES[1].EkaterinaKimMS,etal.CG-806,aFirst-in-ClassPan-FLT3/Pan-BTKInhibitor,ExhibitsBroadSignalingInhibitioninChronicLymphocyticLeukemiaCells.bloodjournalBloodblood(2019).134(Supplement_1):3051.[2].Abstract44:CG′806,afirst-in-classFLT3/BTKinhibitor,exhibitspotentactivityagainstAMLpatientsampleswithmutantorwildtypeFLT3,aswellasotherhematologicmalignancysubtypes[3].GuopanYu,etal.CG'806,aNovelPan-FLT3/BTKMulti-KinaseInhibitor,InducesCellCycleArrest,ApoptosisorAutophagyinAMLCellsDependingonFLT3MutationStatus.Bloodblood(2017).130(Suppl_1):462[4].AptoseBiosciencestoPresentCG’806DataatAACRHematologicMalignanciesMeetingMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.