DCLK1-IN-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEDCLK1-IN-1Cat.No.:HY-135985CASNo.:2222635-15-4分?式:C??H??F?N?O?分?量:527.54作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:35.71mg/mL(67.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8956mL9.4780mL18.9559mL5mM0.3791mL1.8956mL3.7912mL10mM0.1896mL0.9478mL1.8956mL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，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.94mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.94mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性DCLK1-IN-1?種選擇性的、體內(nèi)相容的雙?質(zhì)素樣激酶1DCLK1激酶結(jié)構(gòu)域化學(xué)探針。DCLK1-IN-1抑制DCLK1和DCLK2激酶(結(jié)合和激酶測定IC50分別為:DCLK1=9.5/57.2nM和DCLK2=31/103nM)。DCLK1-IN-1具有低毒性，可以研究DCLK1的?物學(xué)特性，確定其在腫瘤中的作?，如DCLK1+胰腺導(dǎo)管腺癌(PDAC)。體外研究DCLK1-IN-1showsnosignificantactivityagainstERK5,ACK,andLRRK2.DCLK1-IN-1potentlybindsDCLK1inHCT116cells(IC50?=?279?nM).DCLK1-IN-1significantlyinhibitedDCLK1,andweaklyinhibitedERK5,inPATU-8988Tcelllysatesandlivecells[1].體內(nèi)研究DCLK1-IN-1hasafavorablepharmacokineticprofileinmice,withahalf-lifeof2.09?hours,anareaunderthecurveof5,506?h/ng?mland81%oralbioavailability[1].REFERENCES[1].FergusonFM,etal.Discoveryofaselectiveinhibitorofdoublecortinlikekinase1.NatChemBiol.2020Apr6.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;