ATM-3507-trihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEATM-3507trihydrochlorideCat.No.:HY-100948BCASNo.:2438679-30-0分?式:C??H??Cl?FN?O?分?量:721.17作?靶點(diǎn):Myosin作?通路:Cytoskeleton儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(346.66mM;Needultrasonic)H2O:33.33mg/mL(46.22mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.3866mL6.9332mL13.8664mL5mM0.2773mL1.3866mL2.7733mL10mM0.1387mL0.6933mL1.3866mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(2.88mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(2.88mM);ClearsolutionBIOLOGICALACTIVITY?物活性ATM-3507trihydrochloride原肌球蛋?(tropomyosin)的?個(gè)有效抑制劑，其在?類??素瘤細(xì)胞系中的IC50值約為3.83-6.84μM。IC50&TargetIC50:3.83-6.84μM(tropomyosin,inhumanmelanomacelllines)[1].體內(nèi)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