Pirtobrutinib-LOXO-305-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPirtobrutinibCat.No.:HY-131328CASNo.:2101700-15-4Synonyms:LOXO-305分⼦式:C₂₂H₂₁F₄N₅O₃分⼦量:479.43作⽤靶点:Btk作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:50mg/mL(104.29mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0858mL10.4291mL20.8581mL5mM0.4172mL2.0858mL4.1716mL10mM0.2086mL1.0429mL2.0858mL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(storedundernitrogen)。-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%salineSolubility:≥2.5mg/mL(5.21mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.75mg/mL(5.74mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(5.74mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pirtobrutinib(LOXO-305)⼀种⾼选择性和⾮共价的下⼀代BTK抑制剂，可抑制多种BTKC481替代突变。Pirtobrutinib导致⼩⿏异种移植模型中BTK依赖性淋巴瘤肿瘤的消退。Pirtobrutinib对BTK的选择性也是370种其他激酶的300倍以上，并且在1μM时对⾮激酶靶点没有明显的抑制作⽤。体外研究Pirtobrutinibpotentlyinhibitsbothwild-typeBTKandBTKC481S-mediatedkinaseactivitywithnanomolarpotency.PirtobrutinibinhibitsWTBTK(Y223)autophosphorylationwithanIC50of3.68nM.PirtobrutinibinhibitsBTKC481SY223,C481TY223,andC481RY223autophosphorylationwithIC50sof8.45,7.23,and11.73nM,respectively[1].REFERENCES[1].GomezEB,etal.Loxo-305,aHighlySelectiveandNon-CovalentNextGenerationBTKInhibitor,InhibitsDiverseBTKC481SubstitutionMutations[J].Blood,2019,134(Supplement_1):4644-4644.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: