Intoplicine-dimesylate-RP-60475-dimesylate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIntoplicinedimesylateCat.No.:HY-101647ACASNo.:133711-99-6Synonyms:RP60475dimesylate分?式:C??H??N?O?S?分?量:540.65作?靶點(diǎn):Topoisomerase作?通路:CellCycle/DNADamage儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:115mg/mL(212.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8496mL9.2481mL18.4963mL5mM0.3699mL1.8496mL3.6993mL10mM0.1850mL0.9248mL1.8496mL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,awayfrommoistureandlight)。-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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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:≥5.75mg/mL(10.64mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5.75mg/mL(10.64mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5.75mg/mL(10.64mM);ClearsolutionBIOLOGICALACTIVITY?物活性Intoplicine(RP60475)dimesylate，?種7H苯并[e]吡啶并[4,3-b]吲哚系列的抗腫瘤衍?物，?種DNA拓?fù)洚悩?gòu)酶I和II抑制劑。Intoplicinedimesylate與DNA(KA=2x105/M)強(qiáng)烈結(jié)合，從?增加線性DNA的長(zhǎng)度[1][2]。IC50&TargetTopoisomeraseITopoisomeraseII體外研究With1-hourexposuretoIntoplicinedimesylateatfinalconcentrationsof2.5micrograms/mLand10.0micrograms/mL,26%and54%oftheassessablespecimensshowspositiveinvitroresponses,respectively[2].WithcontinuousexposuretoIntoplicinedimesylateatconcentrationsof0.25micrograms/mLand2.5micrograms/mL,16%and71%oftheassessablespecimensshowedpositiveresponses,respectively[2].Activityisseenagainstbreast(71%),non-small-celllung(69%),andovarian(45%)cancercolony-formingunitsataIntoplicinedimesylateconcentrationof10.0micrograms/mLafter1-hourexposure[2].體內(nèi)研究Atthehighestnon-toxicdose(HNTD)(6mg/kg/injection,totaldose,36mg/kg),intoplicinedimesylateshowshighlyactivewithaT/Cof0%andacorrespondingtotallogcellkillof3[3].REFERENCES[1].RiouJF,etal.Intoplicine(RP60475)anditsderivatives,anewclassofantitumoragentsinhibitingbothtopoisomeraseIandIIactivities.CancerRes.1993;53(24):5987-5993.[2].EckardtJR,etal.Activityofintoplicine(RP60475),anewDNAtopoisomeraseIandIIinhibitor,againsthumantumorcolony-formingunitsinvitro.JNatlCancerInst.1994;86(1):30-33.[3].BisseryMC,etal.Antitumoractivityofintoplicine(RP60475,NSC645008),anewbenzo-pyrido-indole:evaluationagainstsolidtumorsandleukemiasinmice.InvestNewDrugs.1993;11(4):263-277.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform