Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMacropa-NH2TFACat.No.:HY-111895BCASNo.:2705054-08-4分?式:C??H??F?N?O??分?量:661.62作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:200mg/mL(302.29mM;Needultrasonic)H2O:100mg/mL(151.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.5114mL7.5572mL15.1144mL5mM0.3023mL1.5114mL3.0229mL10mM0.1511mL0.7557mL1.5114mL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(storedundernitrogen)。-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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(7.56mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥5mg/mL(7.56mM);Clearsolution3.請(qǐng)依序添加每種溶劑：PBSSolubility:100mg/mL(151.14mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Macropa-NH2TFAMacropa-NCS的前體。Macropa-NCS能與曲妥珠單抗以及前列腺特異性膜抗原靶向化合物RPS-070結(jié)合，?種可應(yīng)?于治療軟組織轉(zhuǎn)移瘤的放射性核素[1]。體外研究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].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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