Vorolanib-CM082-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVorolanibCat.No.:HY-109019CASNo.:1013920-15-4Synonyms:CM082;X-82分?式:C??H??FN?O?分?量:439.48作?靶點(diǎn):VEGFR;PDGFR作?通路:ProteinTyrosineKinase/RTK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:27mg/mL(61.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2754mL11.3771mL22.7542mL5mM0.4551mL2.2754mL4.5508mL10mM0.2275mL1.1377mL2.2754mL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：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.25mg/mL(5.12mM);ClearsolutionBIOLOGICALACTIVITY?物活性Vorolanib(CM082)?種具有?服活性的，有效的VEGFR/PDGFR抑制劑。Vorolanib?種有效的ATP結(jié)合盒(ABC)轉(zhuǎn)運(yùn)蛋?抑制劑。Vorolanib?種?管?成抑制劑，與ZD1839(HY-50895)聯(lián)?具有抗腫瘤活性。體外研究Vorolanib(CM082;1-100μM)canspecificallyenhancethesensitivityofasubstratechemotherapeuticalagentinoverexpressingABCG2cells,butnotinoverexpressingABCB1cells.Vorolanib(1.25,2.5,5.0,20μ

M)doesnotinfluencetheexpressionofABCG2inmRNAorproteinLevels[1].Vorolanib(0.001-10μM)inhibitsthegrowthofVEGF‐stimulatedHUVECs(IC50=0.031μM)andFBS‐stimulatedHUVECgrowth(IC50=29.9?μM)[2].Vorolanib(0.01,0.1,1μM)exhibitsaconcentration‐dependentinhibitiononVEGF‐induced(40ng/mL)

phosphorylationofVEGFR2anditsdownstreamsignalingmoleculesERK1/2,AKT,andSTAT3inHUVECs.

Vorolanib(0.1,1μM)inhibitsFBS‐stimulatedtubeformationandcellmigrationofHUVECsinaconcentration‐

dependentmanner[2].體內(nèi)研究Vorolanib(CM082;20mg/kg;gavage;onceevery2days;1hbeforeSKF104864A;for23days)enhancestheanti-tumoreffectofSKF104864A(HY-13768;2mg/kg;i.p.;onceevery2days)onxenograftsofABCG2-overexpressingcells(nudemiceaged5-6weeksandweighing15-17gconstructedbyinjectingH460/MX20cells).Thereisnosignificantdifferenceinthetumorweightandsizeamongthecontrolgroup,theSKF104864Agroup,andtheVorolanibgroup[1].Vorolanib(80mg/kg;twicedaily;for21days)hasantitumoractivitycombinedwithZD1839(10mg/kg;q.d;for21days)onH3255tumorxenograft(femaleBALB/cnudemiceagedfiveweeks)[2].REFERENCES[1].LejiaXu,etal.CM082EnhancestheEfficacyofChemotherapeuticDrugsbyInhibitingtheDrugEffluxFunctionofABCG2.MolTherOncolytics.2019Dec27;16:100-110.[2].KunZhang,etal.CM082,anovelangiogenesisinhibitor,enhancestheantitumoractivityofZD1839onepidermalgrowthfactorreceptormutantnon-smallcelllungcancerinvitroandinvivo.ThoracCancer.2020Jun;11(6):1566-1577.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor