AZ32-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAZ32Cat.No.:HY-112305CASNo.:2288709-96-4分⼦式:C₂₀H₁₆N₄O分⼦量:328.37作⽤靶点:ATM/ATR作⽤通路:CellCycle/DNADamage;PI3K/Akt/mTOR储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥150mg/mL(456.80mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0453mL15.2267mL30.4535mL5mM0.6091mL3.0453mL6.0907mL10mM0.3045mL1.5227mL3.0453mL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:≥2.5mg/mL(7.61mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.61mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.61mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AZ32⼀种⼝服可利⽤的，可穿透⾎脑屏障的ATM抑制剂，IC50IC50为0.31μM。IC50&TargetATMATM6.2nM(IC50)0.31μM(IC50,incell)体外研究AZ32isanext-generationblood-brainbarrier(BBB)-penetratingATMinhibitor.AZ32blockstheDNAdamageresponseandradiosensitizedGBMcellsinvitro[1].体内研究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.