CXD101-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECXD101Cat.No.:HY-100748CASNo.:934828-12-3分⼦式:C₂₄H₂₉N₅O分⼦量:403.52作⽤靶点:HDAC作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥31mg/mL(76.82mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4782mL12.3910mL24.7819mL5mM0.4956mL2.4782mL4.9564mL10mM0.2478mL1.2391mL2.4782mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.20mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.20mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.20mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CXD101⼀种有效的，选择性的，具有⼝服活性的I类HDAC抑制剂，对HDAC1，HDAC2和HDAC3的IC50分别为63nM，570nM和550nM。CXD101对II类HDAC没有活性，并具有抗肿瘤活性。IC50&TargetHDAC1HDAC3HDAC263nM(IC50)550nM(IC50)570nM(IC50)体外研究CXD101hasbeentestedinvitroincolon,lung,non-Hodgkinlymphoma,andmyelomacelllineswithIC50srangedfrom0.2to15μM[2].体内研究CXD101substantiallyreducestumorsizeinmurinexenograftlung(A549a)andcolon(HT29)modelsatadoseof50mg/kg.Tumorreductionsarefoundtobeassociatedwithincreasedhistoneacetylationand

decreasedHDACenzymeactivity[2].ForCXD101,afteroraldosinginmurineandcaninemodels,peakplasmaconcentrations(Cmax)arereached1to2hoursafterthedoseandterminalhalf‐livesare6hoursand8hours,respectively.Aftermurineoral[14C]-CXD101atadoseof1.6mg/kg(4μmol/kg),tissueradioactivitypeaked3to6hoursafterthedoseanddeclinedslowlythereafterwithCXD101‐relatedmaterialstillpresentintissue21daysafterthedose[2].REFERENCES[1].EyreTA,etal.Predictivebiomarkersfordiseasesensitivityinlymphoma-theholygrailforHDACinhibitors?Oncotarget.2018Dec18;9(99):37280-37281.[2].EyreTA,etal.Aphase1studytoassessthesafety,tolerability,andpharmacokineticsofCXD101inpatientswithadvancedcancer.Cancer.2019Jan1;125(1):99-108.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications