ACP-5862-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEACP-5862Cat.No.:HY-135334CASNo.:2230757-47-6分⼦式:C₂₆H₂₃N₇O₃分⼦量:481.51作⽤靶点:DrugMetabolite;Btk;CytochromeP450作⽤通路:MetabolicEnzyme/Protease;ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(519.20mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0768mL10.3840mL20.7680mL5mM0.4154mL2.0768mL4.1536mL10mM0.2077mL1.0384mL2.0768mL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%salineSolubility:≥2.08mg/mL(4.32mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性ACP-5862Acalabrutinib的主活性的，循环的，吡咯烷开环代谢产物，对Bruton酪氨酸激酶(BTK)的IC50为5.0nM。ACP-5862时间依赖性的CYP3A4和CYP2C8弱抑制剂。Acalabrutinib⼀种⼝服有效的，选择性的BTK抑制剂，IC50和EC50分别为3nM和8nM。IC50&TargetCYP2C8CYP3A4体内研究llurineapinroleimlydotwseolthreefldaligrueinthiban,atflfis6.9hoursandthemeanACP-5862(M27)isthemajorsinglemetaboliteinthesystemiccirculationandaccountesfor57.4%and42.1%oftheAUC0-ttotalradioactivityinmaleandfemaleratplasma,respectively.ACP-5862,themajorhumanmetabolite,isarelativelyminorcomponentinthesystemiccirculationandaccountesfor6.1%and8.1%oftheAUC0-ttotalradioactivityinmaleandfemaledogplasma,respectively[1].ACP-5862(1or10μM)hasreversibleproteinbindingof98.6%,99.8%,94.3%,98.6%inmouse,rat,dog,andhumanplasma[1].户使⽤本产品发表的科研⽂献•BiochemBiophysResCommun.2021Jan1;534:995-1002.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HermanSE,etal.TheBruton'styrosinekinase(BTK)inhibitoracalabrutinibdemonstratespotenton-targeteffectsandefficacyintwomousemodelsofchroniclymphocyticleukemia.ClinCancerRes.2016Nov30[2].DiansongZhou,etal.EvaluationoftheDrug-DrugInteractionPotentialofAcalabrutinibandItsActiveMetabolite,ACP-5862,UsingaPhysiologically-BasedPharmacokineticModelingApproach.CPTPharmacometricsSystPharmacol.2019Jul;8(7):489-499.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For