ACP-5862-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEACP-5862Cat.No.:HY-135334CASNo.:2230757-47-6分?式:C??H??N?O?分?量:481.51作?靶點(diǎn):DrugMetabolite;Btk;CytochromeP450作?通路:MetabolicEnzyme/Protease;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:250mg/mL(519.20mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0768mL10.3840mL20.7680mL5mM0.4154mL2.0768mL4.1536mL10mM0.2077mL1.0384mL2.0768mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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(4.32mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性ACP-5862Acalabrutinib的主活性的，循環(huán)的，吡咯烷開(kāi)環(huán)代謝產(chǎn)物，對(duì)Bruton酪氨酸激酶(BTK)的IC50為5.0nM。ACP-5862時(shí)間依賴性的CYP3A4和CYP2C8弱抑制劑。Acalabrutinib?種?服有效的，選擇性的BTK抑制劑，IC50和EC50分別為3nM和8nM。IC50&TargetCYP2C8CYP3A4體內(nèi)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].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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