Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESelpercatinibCat.No.:HY-114370CASNo.:2152628-33-4Synonyms:LOXO-292分?式:C??H??N?O?分?量:525.6作?靶點:RET作?通路:ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:62.5mg/mL(118.91mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9026mL9.5129mL19.0259mL5mM0.3805mL1.9026mL3.8052mL10mM0.1903mL0.9513mL1.9026mL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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(3.96mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.96mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.96mM);ClearsolutionBIOLOGICALACTIVITY?物活性Selpercatinib(LOXO-292)?種有效的選擇性RET激酶抑制劑，抑制RET(WT)，RET(V804M)和RET(G810R)，其IC50值分別為14.0nM，24.1nM和530.7nM。Selpercatinib具有抗腫瘤作?。IC50&TargetIC50:14.0nM(RETWT),24.1nM(RETV804M),and530.7nM(RETG810R)[2]體內(nèi)研究Selpercatinib(LOXO-292;10mg/kg;i.g.;for0-2h)hasgoodpharmacokineticsafteroralgavageinFVB/NRjmice[1].PharmacokineticParametersofSelpercatinibinFVB/NRjmice[1].Administrationi.g.(10mg/kg)Tmax(h)1.8Cmax(ng/mL)7862AUC(ng·h/mL)26649FVB/NRjmice,10mg/kgi.g.[1]AnimalModel:MaleFVB/NRjmice[1]Dosage:10mg/kgAdministration:Oralgavage;for7.5min,15min,30min,1hand2h(PharmacokineticAnalysis)Result:HadgoodpharmacokineticsafteroralgavageinFVB/NRjmice.戶使?本產(chǎn)品發(fā)表的科研?獻?Cancers(Basel).2021,13(8),1909.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].?entürkR,et,al.QuantitativebioanalyticalassayfortheselectiveRETinhibitorsselpercatinibandpralsetinibinmouseplasmaandtissuehomogenatesusingliquidchromatography-tandemmassspectrometry.JChromatogrBAnalytTechnolBiomedLifeSci.[2].StevenW.Andrews,etal.Substitutedpyrazolo[1,5-a]pyridinecompoundsasretkinaseinhibitors.WO2018071447A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr