BIIB068-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBIIB068Cat.No.:HY-131342CASNo.:1798787-27-5分?式:C??H??N?O?分?量:435.52作?靶點(diǎn):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:31.25mg/mL(71.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2961mL11.4805mL22.9611mL5mM0.4592mL2.2961mL4.5922mL10mM0.2296mL1.1481mL2.2961mL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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.78mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.78mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.78mM);ClearsolutionBIOLOGICALACTIVITY?物活性BIIB068?種有效，選擇性，可逆和具有?服活性的BTK抑制劑，IC50為1nM，Kd為0.3nM。BIIB068對(duì)BTK的選擇性?其他激酶?400倍。BIIB068可?于??免疫性疾病的研究。IC50&TargetIC50:1nM(BTK)[1]Kd:0.3nM(BTK)[1]體外研究BIIB068(compound1)improvesthewholebloodcellpotency(humanwholebloodBTKphosphorylation(IC50=0.12μM)[1].BIIB068(compound1;30μM,10μM,3.3μM,and1.1μM)inhibitsBCRmediatedPLCγ2phosphorylationinRamosBcells(IC50=0.4μM),anti-IgDinducedandanti-IgMBCR-inducedBcellactivationinhumanPBMCs(IC50=0.11μMand0.21μM,respectively)[1].BIIB068(compound1)inhibitsFcγR-mediatedROSproductioninneutrophilswithanIC50of54nM[1].體內(nèi)研究BIIB068(compound1)isstableintheplasmaofmouse,rat,beagledog,andcynomolgusmonkey(>95%parentcompoundremainingafter6hoursofincubation)[1].BIIB068(compound1)exhibitsgooddrug-likeproperties(LLE=5)whichresultsinlowinvivoclearance(CL%Qh=6)andmoderateoralbioavailability(%F=48)whendosedinrats.BIIB068(5mg/kg;po)treatmentshowstheT1/2of1.2hours,2.1hoursand0.9hourforrats,dogandcynomolgusmonkey,respectively.BIIB068showsacceptableADME(absorption,distribution,metabolism,andexcretion)properties[1].REFERENCES[1].BinMa,TonikaBohnert,etal.DiscoveryofBIIB068:ASelective,Potent,ReversibleBruton'sTyrosineKinaseInhibitorasanOrallyEfficaciousAgentforAutoimmuneDiseases.JMedChem.2020Jul22.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicati