ATM-3507-trihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEATM-3507trihydrochlorideCat.No.:HY-100948BCASNo.:2438679-30-0分⼦式:C₃₇H₄₉Cl₃FN₅O₂分⼦量:721.17作⽤靶点:Myosin作⽤通路:Cytoskeleton储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:250mg/mL(346.66mM;Needultrasonic)H2O:33.33mg/mL(46.22mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3866mL6.9332mL13.8664mL5mM0.2773mL1.3866mL2.7733mL10mM0.1387mL0.6933mL1.3866mL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(sealedstorage,awayfrommoisture)。-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(2.88mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(2.88mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ATM-3507trihydrochloride原肌球蛋⽩(tropomyosin)的⼀个有效抑制剂，其在⼈类⿊⾊素瘤细胞系中的IC50值约为3.83-6.84μM。IC50&TargetIC50:3.83-6.84μM(tropomyosin,inhumanmelanomacelllines)[1].体内研究Themaximaltolerancedose(MTD)forTR100andATM-3507is60and150mg/kg,respectively.Itisfoundthatasignificantinhibitionoftumorgrowthandprolongationofanimalsurvivalusingeithercombinationcomparedwitheachmonotherapy.Themediansurvivalofmiceincreasedfrom18daysformicetreatedwithATM-3507tomorethan49daysformicetreatedwiththecombination.ItisalsofoundthattwiceweeklyintravenousadministrationofATM-3507alsoshowcombinationefficacy.Theimpactofeachtreatmentorthecombinationonbodyweightisminimal.DruglevelsaremeasuredfollowingtheintravenousadministrationofATM-3507at30mg/kginBalb/cmice(n=3pertimepoint).Themeanhalf-lifeofATM-3507is5.01hrsfortheterminaleliminationphase.ThemeanAUC0-tintheplasmais14,548ng/h/mL.TheCmaxofATM-3507is5,758ng/mLandthethet1/2is5.01h.TheobservedplasmaclearanceandvolumeofdistributionatsteadystateofATM-3507is33.8mL/min/kgand7.23L/kg,respectively[1].REFERENCES[1].CurrierMA,etal.IdentificationofCancer-TargetedTropomyosinInhibitorsandTheirSynergywithMicrotubuleDrugs.MolCancerTher.2017Aug;16(8):1555-1565.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio