Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEThailanstatinACat.No.:HY-129589CASNo.:1426953-21-0分?式:C??H??NO?分?量:535.63作?靶點(diǎn):ADCCytotoxin作?通路:Antibody-drugConjugate/ADCRelated儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(466.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8670mL9.3348mL18.6696mL5mM0.3734mL1.8670mL3.7339mL10mM0.1867mL0.9335mL1.8670mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.88mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.88mM);ClearsolutionBIOLOGICALACTIVITY?物活性ThailanstatinA?種有效的真核RNA剪接(RNAsplicing)抑制劑(IC50=650nM)。ThailanstatinA通過?共價(jià)結(jié)合到剪接體的U2snRNA亞復(fù)合物的SF3b亞單位發(fā)揮作?，并且對多種癌細(xì)胞系顯?低nM到亞nM的IC50值。ThailanstatinA與Trastuzumab上的賴氨酸結(jié)合，可產(chǎn)?“?連接?(linker-less)”ADC。體外研究ThailanstatinA(TST-A)isapotentantiproliferativenaturalproductdiscoveredbyourgroupfromBurkholderiathailandensisMSMB43[2].ThailanstatinA(DU-145,NCI-H232A,MDA-MB-231andSKOV-3cells)exhibitspotentantiproliferativeactivitieswithGI50sinthesinglenMrange(1.11-2.69nM)[3].REFERENCES[1].PuthenveetilS,etal.NaturalProductSplicingInhibitors:ANewClassofAntibody-DrugConjugate(ADC)Payloads.BioconjugChem.2016;27(8):1880-1888.[2].GhoshAK,etal.EnantioselectiveSynthesisofThailanstatinAMethylEsterandEvaluationofinVitroSplicingInhibition.JOrgChem.2018;83(9):5187-5198.[3].LiuX,etal.Genomics-guideddiscoveryofthailanstatinsA,B,andCAspre-mRNAsplicinginhibitorsandantiproliferativeagentsfromBurkholderiathailandensisMSMB43.JNatProd.2013;76(4):685-693.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl