N-Deshydroxyethyl-Dasatinib-N-Deshydroxyethyl-BMS-354825-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEN-DeshydroxyethylDasatinibCat.No.:HY-107447CASNo.:910297-51-7Synonyms:N-DeshydroxyethylBMS-354825分?式:C??H??ClN?OS分?量:443.95作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:55mg/mL(123.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2525mL11.2625mL22.5251mL5mM0.4505mL2.2525mL4.5050mL10mM0.2253mL1.1263mL2.2525mL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。-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>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.75mg/mL(6.19mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(6.19mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(6.19mM);ClearsolutionBIOLOGICALACTIVITY?物活性N-DeshydroxyethylDasatinib(N-DeshydroxyethylBMS-354825)Dasatinib的代謝物，Dasatinib?種多激酶抑制劑，能有效抑制Bcr-Abl、Src家族和??板衍??長(zhǎng)因?受體激酶，N-DeshydroxyethylDasatinib可?于癌癥和免疫疾病的研究。體內(nèi)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