Macropa-NH2-TFA-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMacropa-NH2TFACat.No.:HY-111895BCASNo.:2705054-08-4分⼦式:C₂₈H₃₈F₃N₅O₁₀分⼦量:661.62作⽤靶点:Others作⽤通路:Others储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:200mg/mL(302.29mM;Needultrasonic)H2O:100mg/mL(151.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5114mL7.5572mL15.1144mL5mM0.3023mL1.5114mL3.0229mL10mM0.1511mL0.7557mL1.5114mL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(storedundernitrogen)。-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>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(7.56mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥5mg/mL(7.56mM);Clearsolution3.请依序添加每种溶剂：PBSSolubility:100mg/mL(151.14mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Macropa-NH2TFAMacropa-NCS的前体。Macropa-NCS能与曲妥珠单抗以及前列腺特异性膜抗原靶向化合物RPS-070结合，⼀种可应⽤于治疗软组织转移瘤的放射性核素[1]。体外研究Awhitesuspensionof11•4TFA(0.1598g,0.16mmol)andNa2CO3(0.2540g,2.4mmol)washeatedatrefluxinacetone(10mL)for30minbeforetheslowadditionofCSCl2(305µLofCSCl2,85%,AcrosOrganics).Theresultingorangesuspensionwasheatedatrefluxfor3handthenconcentratedat30°Cunderreducedpressuretoapale-orangesolid.Thesolidwasdissolvedportionwisein10%ACN/H2Ocontaining0.2%TFA(8mLtotal),filtered,andimmediatelypurifiedbypreparativeHPLCusingMethodC.Purefractionswerecombined,concentratedatRTunderreducedpressuretoremovetheorganicsolvent,andthenlyophilized.Fractionsthatwerenotabletobeconcentratedimmediatelywerefrozenat-80°C.Isothiocyanate12wasobtainedasamixtureofwhiteandpale-yellowsolid(0.0547g)andwasstoredat–80°CinajarofDrierite.Astocksolutioncontaining4.4mg/mLofmacropa-NCSwaspreparedin0.1MpH9.1NaHCO3buffercontaining0.154MNaClandwasstoredat-80°C.ToaportionofTmabinsaline(74μL)wereaddedmacropa-NCS(52μL)andNaHCO3buffer(266μL),sothatthefinalconcentrationsofTmabandmacropa-NCSwere5.1mg/mLand0.59mg/mL,respectively.Macropa-NCSwasestimatedtobein16-foldmolarexcesstoTmabbasedonamolecularweightof1045.76g/molformacropa-NCS(tetra-TFAsalt)[1].户使⽤本产品发表的科研⽂献•JNuclMed.2021Aug12;jnumed.121.262459.•SciRep.2020Dec17;10(1):22203.•Patent.US20210236667A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ThieleNA,etal.AnEighteen-MemberedMacrocyclicLigandforActinium-225TargetedAlphaTherapy.AngewChemIntEdEngl.2017;56(46):14712-14717.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo