DCLK1-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEDCLK1-IN-1Cat.No.:HY-135985CASNo.:2222635-15-4分⼦式:C₂₆H₂₈F₃N₇O₂分⼦量:527.54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:35.71mg/mL(67.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8956mL9.4780mL18.9559mL5mM0.3791mL1.8956mL3.7912mL10mM0.1896mL0.9478mL1.8956mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.94mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.94mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性DCLK1-IN-1⼀种选择性的、体内相容的双⽪质素样激酶1DCLK1激酶结构域化学探针。DCLK1-IN-1抑制DCLK1和DCLK2激酶(结合和激酶测定IC50分别为:DCLK1=9.5/57.2nM和DCLK2=31/103nM)。DCLK1-IN-1具有低毒性，可以研究DCLK1的⽣物学特性，确定其在肿瘤中的作⽤，如DCLK1+胰腺导管腺癌(PDAC)。体外研究DCLK1-IN-1showsnosignificantactivityagainstERK5,ACK,andLRRK2.DCLK1-IN-1potentlybindsDCLK1inHCT116cells(IC50ꢀ=ꢀ279ꢀnM).DCLK1-IN-1significantlyinhibitedDCLK1,andweaklyinhibitedERK5,inPATU-8988Tcelllysatesandlivecells[1].体内研究DCLK1-IN-1hasafavorablepharmacokineticprofileinmice,withahalf-lifeof2.09ꢀhours,anareaunderthecurveof5,506ꢀh/ngꢀmland81%oralbioavailability[1].REFERENCES[1].FergusonFM,etal.Discoveryofaselectiveinhibitorofdoublecortinlikekinase1.NatChemBiol.2020Apr6.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;