AZ32-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAZ32Cat.No.:HY-112305CASNo.:2288709-96-4分?式:C??H??N?O分?量:328.37作?靶點(diǎn):ATM/ATR作?通路:CellCycle/DNADamage;PI3K/Akt/mTOR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:≥150mg/mL(456.80mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0453mL15.2267mL30.4535mL5mM0.6091mL3.0453mL6.0907mL10mM0.3045mL1.5227mL3.0453mL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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.61mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.61mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.61mM);ClearsolutionBIOLOGICALACTIVITY?物活性AZ32?種?服可利?的，可穿透?腦屏障的ATM抑制劑，IC50IC50為0.31μM。IC50&TargetATMATM6.2nM(IC50)0.31μM(IC50,incell)體外研究AZ32isanext-generationblood-brainbarrier(BBB)-penetratingATMinhibitor.AZ32blockstheDNAdamageresponseandradiosensitizedGBMcellsinvitro[1].體內(nèi)研究AZ32,withenhancedBBBpenetration,ishighlyefficientinvivoasradiosensitizerinsyngeneicandhuman,orthotopicmousegliomamodelcomparedwithAZ31.AZ32isaspecificinhibitoroftheATMkinasethatpossessesgoodBBBpenetrationinmouse.FollowingasingleoraldoseofAZ32(200mg/kg)inmice,thefree-brainconcentrationsofAZ32areinexcessofthecellularIC50forapproximately22hours[1].REFERENCES[1].KarlinJ,etal.OrallyBioavailableandBlood-BrainBarrier-PenetratingATMInhibitor(AZ32)RadiosensitizesIntracranialGliomasinMice.MolCancerTher.2018Aug;17(8):1637-1647.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.