Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesKMH-233Cat.No.:HY-120139CASNo.:1941174-13-5分?式:C??H??N?O?分?量:587.58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:90mg/mL(153.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7019mL8.5095mL17.0190mL5mM0.3404mL1.7019mL3.4038mL10mM0.1702mL0.8509mL1.7019mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶1.請(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.25mg/mL(3.83mM);Clearsolution此?案可獲得≥2.25mg/mL(3.83mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL22.5mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請(qǐng)依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:2.25mg/mL(3.83mM);Suspendedsolution;Needultrasonic1/3此?案可獲得2.25mg/mL(3.83mM)的均勻懸濁液，懸濁液可?于?服和腹腔注射。以1mL?作液為例，取100μL22.5mg/mL的澄DMSO儲(chǔ)備液加到900μL20%的SBE-β-CD?理鹽??溶液中，混合均勻。BIOLOGICALACTIVITY?物活性KMH-233?種有效，可逆的且選擇性的l型氨酸轉(zhuǎn)運(yùn)蛋?1(LAT1)抑制劑，可抑制LAT1底物，l-leucin的攝取(IC50=18μM)以及細(xì)胞?長(zhǎng)。即使在低濃度(25μM)下，KMH-233仍可顯增強(qiáng)Bestatin和鉑的療效。體外研究KMH-233isabletoinhibitbindingandtransportofessentialneutralaminoacidsandthus,inhibitthecellgrowthofcancercells[1].KMH-233showsasignificantreductionofcellgrowthwithanIC50of124μM[1].KMH-233iseffectiveandabletopotentiatetheanti-proliferativeefficacyofBestatin(100μM)andCisplatin(100μM)atalowerconcentrationof25μM,inhibitingcellgrowth53%and50%,respectively[1].CellProliferationAssay[1]CellLine:MCF-7cellsConcentration:0.5-1000μMIncubationTime:72hoursResult:ShowedasignificantreductionofcellgrowthwithanIC50of124μM.REFERENCES[1].HuttunenKM,etal.ASelectiveandSlowlyReversibleInhibitorofl-TypeAminoAcidTransporter1(LAT1)PotentiatesAntiproliferativeDrugEfficacyinCancerCells.JMedChem.2016;59(12):5740-5751.McePdfHeight2/3MedChemExpress(MCE)只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研