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

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEMacropa-NH2TFACat.No.:HY-111895B分⼦式:C₂₈H₃₈F₃N₅O₁₀分⼦量:661.62作⽤靶点:Others作⽤通路:Others储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCOA.溶解性数据体外实验DMSO:200mg/mL(302.29mM;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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：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%cornoilSolubility:≥5mg/mL(7.56mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE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].REFERENCES[1].ThieleNA,etal.AnEighteen-MemberedMacrocyclicLigandforActinium-225TargetedAlphaTherapy.AngewChemIntEdEngl.2017;56(46):14712-14717.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical/