Selpercatinib-LOXO-292-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESelpercatinibCat.No.:HY-114370CASNo.:2152628-33-4Synonyms:LOXO-292分⼦式:C₂₉H₃₁N₇O₃分⼦量:525.6作⽤靶点:RET作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(118.91mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9026mL9.5129mL19.0259mL5mM0.3805mL1.9026mL3.8052mL10mM0.1903mL0.9513mL1.9026mL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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(3.96mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.96mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.96mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Selpercatinib(LOXO-292)⼀种有效的选择性RET激酶抑制剂，抑制RET(WT)，RET(V804M)和RET(G810R)，其IC50值分别为14.0nM，24.1nM和530.7nM。Selpercatinib具有抗肿瘤作⽤。IC50&TargetIC50:14.0nM(RETWT),24.1nM(RETV804M),and530.7nM(RETG810R)[2]体内研究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.户使⽤本产品发表的科研⽂献•Cancers(Basel).2021,13(8),1909.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ŞentürkR,et,al.QuantitativebioanalyticalassayfortheselectiveRETinhibitorsselpercatinibandpralsetinibinmouseplasmaandtissuehomogenatesusingliquidchromatography-tandemmassspectrometry.JChromatogrBAnalytTechnolBiomedLifeSci.[2].StevenW.Andrews,etal.Substitutedpyrazolo[1,5-a]pyridinecompoundsasretkinaseinhibitors.WO2018071447A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr