Chiauranib-CS2164-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEChiauranibCat.No.:HY-124526CASNo.:1256349-48-0Synonyms:CS2164分⼦式:C₂₇H₂₁N₃O₃分⼦量:435.47作⽤靶点:VEGFR;PDGFR;c-Kit;AuroraKinase;c-Fms作⽤通路:ProteinTyrosineKinase/RTK;CellCycle/DNADamage;Epigenetics储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:62.5mg/mL(143.52mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2964mL11.4818mL22.9637mL5mM0.4593mL2.2964mL4.5927mL10mM0.2296mL1.1482mL2.2964mL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(protectfromlight)。-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>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.78mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Chiauranib(CS2164)⼀种针对肿瘤⾎管⽣成的具有⼝服活性的多靶点抑制剂。Chiauranib有效抑制⾎管⽣成相关激酶(VEGFR1，VEGFR2，VEGFR3，PDGFRα和c-Kit)，有丝分裂相关激酶AuroraB和慢性炎症相关激酶CSF-1R，IC50值为1-9nM。Chiauranib具有很强的抗癌作⽤。IC50&TargetFlt-1KDRFlt-4PDGFRα8nM(IC50)7nM(IC50)9nM(IC50)1nM(IC50)AuroraBPDGFRβc-KitCSF-1R9nM(IC50)93nM(IC50)4nM(IC50)7nM(IC50)体外研究Chiauranib(CS2164;3μM;24hours)showsinductionofG2/McellcyclearrestandsuppressionofcellproliferationintumortissuesthroughtheinhibitionofAuroraB-mediatedH3phosphorylation[1].InHUVECandPDGFRβphosphorylationinPDGFRβoverexpressedNIH3T3cells,Chiauranib(CS2164;0.03-3μM)displaysanti-angiogenicactivitiesthroughsuppressionofVEGFR/PDGFRphosphorylation,inhibitionofligand-dependentcellproliferationandcapillarytubeformation,andpreventionofvasculatureformationintumortissues[1]..Chiauranib(CS2164)inhibitsCSF-1Rphosphorylationthatleadstothesuppressionofligand-stimulatedmonocyte-to-macrophagedifferentiationandreducesCSF-1R+cellsintumortissues[1].CellCycleAnalysis[1]CellLine:Molt-4cellsConcentration:3μMIncubationTime:24hoursResult:InducedthepronouncedcellcyclearrestintheG2/Mphaseat3μM.WesternBlotAnalysis[1]CellLine:Molt-4cellsConcentration:1.5μM,3μM,6μMIncubationTime:24hoursResult:iepeldenthintialreductioninthelevelofp-H3inMolt‐4cellsinaconcentration-体内研究Chiauranib(CS2164;0.5-40mg/kg;oraladministration;oncedaily;for33daysor43days)treatmentinducesremarkableregressionorcompleteinhibitionoftumorgrowthatwell-toleratedoraldosesinseveralhuman2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEtumorxenograftmodels.Chiauranibexhibitsbroadandpotentinvivoanti-tumoractivities[1].AnimalModel:FemaleBALB/cathymic(nu+/nu+)mice(6-weekold)bearingHCT-8,SMMC-7721,MGC‐803orA549cells[1]Dosage:2.5mg/kg,5mg/kg,10mg/kg,20mg/kg,40mg/kgAdministration:Oraladministration;oncedaily;for33daysor43daysResult:Inducedremarkableregressionorcompleteinhibitionoftumorgrowthinseveralhumantumorxenograftmodels.REFERENCES[1].YouZhou,etal.CS2164,anovelmulti-targetinhibitoragainsttumorangiogenesis,mitosisandchronicinflammationwithanti-tumorpotency.CancerSci.2017Mar;108(3):469-477.McePdfHeightCaution:Producthasnot