Pirtobrutinib-LOXO-305-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPirtobrutinibCat.No.:HY-131328CASNo.:2101700-15-4Synonyms:LOXO-305分?式:C??H??F?N?O?分?量:479.43作?靶點(diǎn):Btk作?通路:ProteinTyrosineKinase/RTK儲存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(104.29mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0858mL10.4291mL20.8581mL5mM0.4172mL2.0858mL4.1716mL10mM0.2086mL1.0429mL2.0858mL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(fù)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(storedundernitrogen)。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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%salineSolubility:≥2.5mg/mL(5.21mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.75mg/mL(5.74mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(5.74mM);ClearsolutionBIOLOGICALACTIVITY?物活性Pirtobrutinib(LOXO-305)?種?選擇性和?共價(jià)的下?代BTK抑制劑，可抑制多種BTKC481替代突變。Pirtobrutinib導(dǎo)致??異種移植模型中BTK依賴性淋巴瘤腫瘤的消退。Pirtobrutinib對BTK的選擇性也是370種其他激酶的300倍以上，并且在1μM時對?激酶靶點(diǎn)沒有明顯的抑制作?。體外研究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: