Thailanstatin-A-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEThailanstatinACat.No.:HY-129589CASNo.:1426953-21-0分⼦式:C₂₈H₄₁NO₉分⼦量:535.63作⽤靶点:ADCCytotoxin作⽤通路:Antibody-drugConjugate/ADCRelated储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(466.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8670mL9.3348mL18.6696mL5mM0.3734mL1.8670mL3.7339mL10mM0.1867mL0.9335mL1.8670mL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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.88mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.88mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ThailanstatinA⼀种有效的真核RNA剪接(RNAsplicing)抑制剂(IC50=650nM)。ThailanstatinA通过⾮共价结合到剪接体的U2snRNA亚复合物的SF3b亚单位发挥作⽤，并且对多种癌细胞系显⽰低nM到亚nM的IC50值。ThailanstatinA与Trastuzumab上的赖氨酸结合，可产⽣“⽆连接⼦(linker-less)”ADC。体外研究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