Darovasertib-LXS196-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDarovasertibCat.No.:HY-101569CASNo.:1874276-76-2Synonyms:LXS196;IDE196分?式:C??H??F?N?O分?量:472.47作?靶點(diǎn):PKC作?通路:Epigenetics;TGF-beta/Smad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:25mg/mL(52.91mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1165mL10.5827mL21.1654mL5mM0.4233mL2.1165mL4.2331mL10mM0.2117mL1.0583mL2.1165mL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：1%DMSO>>99%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:0.33mg/mL(0.70mM);Suspendedsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.29mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.29mM);Clearsolution4.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.29mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥1.67mg/mL(3.53mM);Clearsolution6.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥1.67mg/mL(3.53mM);ClearsolutionBIOLOGICALACTIVITY?物活性Darovasertib(LXS196)有效的、選擇性的和具有?服活性的蛋?激酶C(PKC)抑制劑，對(duì)PKCα、PKCθ和GSK3β的IC50值分別為1.9nM、0.4nM和3.1μM。Darovasertib有潛??于葡萄膜?素瘤的研究。IC50&TargetPKCαPKCθGSK3β1.9nM(IC50)0.4nM(IC50)3.1μM(IC50)體外研究Uponoraladministration,proteinkinaseCinhibitorLXS196bindstoandinhibitsPKC,whichpreventstheactivationofPKC-mediatedsignalingpathways.Thismayleadtotheinductionofcellcyclearrestandapoptosisinsusceptibletumorcells.PKC,aserine/threonineproteinkinaseoverexpressedincertaintypesofcancercells,isinvolvedintumorcelldifferentiation,proliferation,invasionandsurvival[1].體內(nèi)研究Darovasertib(LXS196;compound9)(15,30,75,150mg/kg,P.O.,mice)showsimprovedefficacy(regression)ina92.1GNAQuvealmelanomaxenograftmodelinadose-dependentlymanner[2].AnimalModel:Miceimplantedwith92.1GNAQmutantuvealmelanomacells[2].Dosage:15,30,75,150mg/kgAdministration:P.O.(bid)for35daysResult:Dose-dependentlysuppressedthetumorgrowth.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Patent.US20210230154A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].ProteinKinaseCInhibitorLXS196[2].US20180179181.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap