N-Deshydroxyethyl-Dasatinib-N-Deshydroxyethyl-BMS-354825-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEN-DeshydroxyethylDasatinibCat.No.:HY-107447CASNo.:910297-51-7Synonyms:N-DeshydroxyethylBMS-354825分⼦式:C₂₀H₂₂ClN₇OS分⼦量:443.95作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:55mg/mL(123.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2525mL11.2625mL22.5251mL5mM0.4505mL2.2525mL4.5050mL10mM0.2253mL1.1263mL2.2525mL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>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.75mg/mL(6.19mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(6.19mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(6.19mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性N-DeshydroxyethylDasatinib(N-DeshydroxyethylBMS-354825)Dasatinib的代谢物，Dasatinib⼀种多激酶抑制剂，能有效抑制Bcr-Abl、Src家族和⾎⼩板衍⽣⽣长因⼦受体激酶，N-DeshydroxyethylDasatinib可⽤于癌症和免疫疾病的研究。体内研究1.19PharmacokineticParametersofN-DeshydroxyethylDasatinibinWistarRats[2].AnalyteCmax(ng/mL)AUC0-t(h*ng/mL)AUC0-inf(h*ng/mL)Tmax(h)T1/2(h)Kel(h-1)N-DeshydroxyethylDasatinib2.058.723.92.010.2930.072REFERENCES[1].ThappaliSR,etal.Simultaneousdeterminationofmethotrexate,dasatinibanditsactivemetaboliteN-deshydroxyethyldasatinibinratplasmabyLC-MS/MS:methodvalidationandapplicationtopharmacokineticstudy.Arzneimittelforschung.2012Dec;62(12):[2].ShibataN,etal.DevelopmentofproteindegradationinducersofoncogenicBCR-ABLproteinbyconjugationofABLkinaseinhibitorsandIAPligands.CancerSci.2017Aug;108(8):1657-1666.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T