CP-609754-LNK-754-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECP-609754Cat.No.:HY-16373CASNo.:1190094-64-4Synonyms:LNK-754;OSI-754分?式:C??H??ClN?O?分?量:479.96作?靶點(diǎn):FarnesylTransferase作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(208.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0835mL10.4175mL20.8351mL5mM0.4167mL2.0835mL4.1670mL10mM0.2084mL1.0418mL2.0835mL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。-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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.21mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.21mM);ClearsolutionBIOLOGICALACTIVITY?物活性CP-609754(LNK-754)?種有效且可逆的法尼轉(zhuǎn)移酶(farnesyltransferase)抑制劑，具有潛在的抗癌活性。CP-609754抑制重組?H-Ras和重組K-Ras法尼化的IC50分別為0.57ng/mL和46ng/mL[1]。體外研究CP-609754(CP-609,754)isareversibleinhibitoroffarnesyltransferasewithaslowon/offrate.CP-609,754inhibitsfarnesylation(IC50=1.72ng/mL)ofmutantH-Rasin3T3H-ras(61L)-transfectedcelllineswithSDSanalysisof[35S]methionine-labeledmaterial[1].CP-609754iscompetitivefortheprenylacceptor(H-Rasprotein)andnoncompetitivefortheprenyldonorfarnesylPPI.CP-609754interactswiththefarnesyltransferase-farnesylPPIcomplexandcompetesforthebindingoftheRasprotein.CP-609754selectivelyinhibitsfarnesylationofbothH-andK-Rasproteinsin3T3transfectants[1].體內(nèi)研究CP-609754(CP-609,754)hasantitumoractivityagainst3T3H-ras(61L)tumorsinvivo[1].WithtwicedailyoraldosingofCP-609754,tumorregressionisachievedwithadoseof100mg/kg;theED50fortumorgrowthinhibitionis28mg/kg[1].Withcontinuousi.p.infusionofCP-609754,tumorgrowthisinhibitedby>50%,andtumorfarnesyltransferaseactivityinhibitedby>30%inmiceinwhichtheplasmaconcentrationofCP-609754ismaintainedabove118ng/mL[1].REFERENCES[1].StacyLMoulder,etal.AphaseIopenlabelstudyofthefarnesyltransferaseinhibitorCP-609,754inpatientswithadvancedmalignanttumors.ClinCancerRes.2004Nov1;10(21):7127-35.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F