Safimaltib-JNJ-67856633-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESafimaltibCat.No.:HY-139399CASNo.:2230273-76-2Synonyms:JNJ-67856633分⼦式:C₂₀H₁₁F₆N₅O₂分⼦量:467.32作⽤靶点:MALT1作⽤通路:MetabolicEnzyme/Protease;NF-κB储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(267.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1399mL10.6993mL21.3986mL5mM0.4280mL2.1399mL4.2797mL10mM0.2140mL1.0699mL2.1399mL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(4.45mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.45mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.45mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Safimaltib(JNJ-67856633)⼀种具有⼝服活性、第⼀类、有效、选择性和变构性MALT1protease抑制剂。Safimaltib在某些情况下导致肿瘤停滞[1][2][3]。IC50&TargetMALT1protease[1][2][3]体外研究Safimaltib(JNJ-67856633)iseffectiveandhighlybioavailableinbothmouseandrattumors,andinsomecasesledtotumorstasis.SafimaltibleadstopotentinvivopharmacodynamicshutdowninCD79b-aswellasCARD11-mutantABC-DLBCLmodelsasmeasuredbyserumIL10oruncleavedBCL10levelsintumors[1][3].体内研究DosedependentinhibitionofthegenerationofTregs(CD4+CD25+FoxP3+)followingCD3/28stimulationwasobservedupontreatmentwithJNJ-67856633suggestingapotentialimmunemodulatoryroleofMALT1inhibition[3].REFERENCES[1].Virtualmeetingdeliversfirsttimedrugstructures[2].APhase1,First-in-Human,Open-LabelStudyoftheSafety,Pharmacokinetics,andPharmacodynamicsofJNJ-67856633,anInhibitorofMALT1,inParticipantswithNHLandCLL[3].Abstract5690:DiscoveryofJNJ-67856633:Anovel,first-in-classMALT1proteaseinhibitorforthetreatmentofBcelllymphomasMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu