SBP-7455-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESBP-7455Cat.No.:HY-137742CASNo.:1884222-74-5分⼦式:C₁₆H₁₇F₃N₄O₂分⼦量:354.33作⽤靶点:ULK;Autophagy作⽤通路:Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(352.78mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8222mL14.1111mL28.2223mL5mM0.5644mL2.8222mL5.6445mL10mM0.2822mL1.4111mL2.8222mL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%salineSolubility:≥2.08mg/mL(5.87mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.87mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SBP-7455⼀种有效的，⾼亲和⼒，具有⼝服活性的双重ULK1/ULK2⾃噬抑制剂，在ADP-Glo分析中的IC50分别为13nM和476nM。SBP-7455有效抑制ULK1/2酶活性，并可⽤于三性乳腺癌(TNBC)的研究。IC50&TargetULK1ULK213nM(IC50)476nM(IC50)体外研究SBP-7455(compound26;72h)treatmentinhibitscellgrowthwithanIC50of0.3μMforMDA-MB-468cells.SBP-7455inhibitsstarvation-inducedautophagicfluxinTNBCcellsthataredependentonautophagyforsurvival[1].体内研究AsingledoseofSBP-7455(compound26)(30mg/kg)isorallyadministeredtomice.TheTmaxforSBP-7455isapproximately1h,theCmaxis990nMandtheT1/2is1.7h.TheplasmaconcentrationofSBP-7455remainsabovetheULK1IC50foralmost4hafteroraldosing[1].ThemicearedosedwithSBP-7455(compound26)(10mg/kg)byoralgavage,andliversampleswerecollectedafter2h.TheresultsrevealsrobustinhibitionofpATG13(Ser318),aswellasdownregulationoftotalATG13andULK1levelsbySBP-7455[1].REFERENCES[1].HuiyuRen,etal.Design,Synthesis,andCharacterizationofanOrallyActiveDual-SpecificULK1/2AutophagyInhibitorthatSynergizeswiththePARPInhibitorOlaparibfortheTreatmentofTriple-NegativeBreastCancer.JMedChem.2020Dec10;63(23):14609-14625McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch