PD-L1-IN-5-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEPD-L1-IN-5Cat.No.:HY-162357CASNo.:2597056-85-2分子式:C₄₀H₄₄ClFN₄O₈分子量:763.25作用靶点:PD-1/PD-L1作用通路:Immunology/Inflammation储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PD-L1-IN-5(X22)是一个口服活性的PD-L1抑制剂，IC50值为785.6nM。PD-L1-IN-5具有体内抗肿瘤活性[1]。体外研究PD-L1-IN-5(X22)(0-150μM,12h)hasnoobviouscytotoxiceffectonMC38andCT26cellsinvitro[1].体内研究PD-L1-IN-5(X22)(0-50mg/kg/dayfor20days,p.o.)demonstratessignificantantitumorefficacyinmurinemodelsofMC38andCT26coloncancerthroughtheupregulationoftumorinfiltrationandcytotoxicityofCD8Tcellspartially,butexhibitslowantitumoreffectinthesyngeneicCT26colorectalcancermodelinimmunodeficientnudemicewhichindicatedthattheantitumormechanismreliesontheimmunesystem[1].PharmacokineticAnalysisinSDratsandC57blo/6mice[1]AnimalmodelRouteDose(mg/kg)t1/2(h)Tmax(h)Cmax(ng/mL)AUC0-t(ng·h/mL)CL(mL/h/kg)F(%)SDratp.o.454.34.0049.8405.6/3.4C57blo/6micep.o.101.60.7255.7315.6/11.5AnimalModel:MC38andCT26tumormousemodel,Balb/cmice(female,8weekold)[1]Dosage:0-50mg/kg/dayfor20daysAdministration:p.o.Result:Inhibitedcolontumorgrowthinmicewithtumorgrowthinhibitionrates(TGI)of49.5%and73.6%atdosesof5mg/kgand25mg/kg,respectively.REFERENCES1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemELiuL,etal.DiscoveryofNovelPD-L1Small-MolecularInhibitorswithPotentInVivoAnti-tumorImmuneActivity.JMedChem.2024Mar28;67(6):4977-4997.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-5