Ro5-3335-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERo5-3335Cat.No.:HY-108470CASNo.:30195-30-3分⼦式:C₁₃H₁₀ClN₃O分⼦量:259.69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:100mg/mL(385.07mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.8507mL19.2537mL38.5075mL5mM0.7701mL3.8507mL7.7015mL10mM0.3851mL1.9254mL3.8507mL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:≥2.5mg/mL(9.63mM);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:≥2.5mg/mL(9.63mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Ro5-3335⼀种苯⼆氮化合物，能作为核⼼结合因⼦(CBF)⽩⾎病抑制剂。Ro5-3335RUNX1-CBFβ相互作⽤抑制剂，可抑制RUNX1/CBFB依赖性反式激活[1]。IC50&TargetRUNX1-CBFβinteraction[1]体外研究Ro5-3335hasantiproliferativeactivityagainsthumanCBFleukemiacelllines,withIC50sof1.1μM,21.7μMand17.3μMforME-1,Kasumi-1andREH,respectively[1].Ro5-3335inhibitsdefinitivehematopoiesisinzebrafishembryos[1].Ro5-3335doesnotcompletelybreakapartRUNX1-CBFβinteraction,butchangestheconformationoftheircomplexorincreasesthedistancebetweenRUNX1andCBFβinthecomplex[1].体内研究Ro5-3335isidentifiedasaninhibitorofRUNX1–CBFβfunctioninzebrafishmodels[1].Ro5-3335rescuespreleukemicphenotypeinaRUNX1-ETOtransgeniczebrafish[1].Ro5-3335(300mg/kg/d;p.o;for30days)reducesleukemiaburdeninamouseCBFB-MYH11leukemiamodel[1].AnimalModel:C57BL/6mice(leukemicmodel)[1]Dosage:300mg/kgAdministration:Oraladministration;daily;for30daysResult:Reducedthenumberofc-kit+cellsinthetransplantedmiceandleukemiccellinfiltrationinthelivers,bonemarrowandspleen.REFERENCES[1].CunninghamL,etal.IdentificationofbenzodiazepineRo5-3335asaninhibitorofCBFleukemiathroughquantitativehighthroughputscreenagainstRUNX1-CBFβinteraction.ProcNatlAcadSciUSA.2012Sep4;109(36):14592-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese