PND-1186-hydrochloride-VS-4718-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPND-1186hydrochlorideCat.No.:HY-13917ACASNo.:1356154-94-3Synonyms:VS-4718hydrochloride;SR-2516hydrochloride分?式:C??H??ClF?N?O?分?量:537.96作?靶點:FAK;Apoptosis作?通路:ProteinTyrosineKinase/RTK;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:200mg/mL(371.77mM;Needultrasonic)H2O:20mg/mL(37.18mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8589mL9.2944mL18.5887mL5mM0.3718mL1.8589mL3.7177mL10mM0.1859mL0.9294mL1.8589mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(9.29mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(9.29mM);ClearsolutionBIOLOGICALACTIVITY?物活性PND-1186hydrochloride(VS-4718hydrochloride)?種有效的，?特異性的，可逆的FAK抑制劑，IC50為1.5nM。PND-1186hydrochloride選擇性促進(jìn)腫瘤細(xì)胞凋亡(apoptosis)[1]。體外研究PND-1186hasanIC50of~100nMinbreastcarcinomacellsasdeterminedbyanti-phospho-specificimmunoblottingtoFAKTyr-397[1].Inmurine4T1breastcarcinomacells,FAKisimportantinpromotinganinvasiveandmetastaticcellphenotype.IncreasingconcentrationsofPND-1186(0.1to1.0μM)addedto4T1cellsinhibitsFAKTyr-397phosphorylation(pY397)andresultsinelevatedlevelsoftotalFAKproteinwithin1h[1].WesternBlotAnalysis[1]CellLine:4T1breastcarcinomacellsConcentration:0.1,0.2,0.4,0.6and1.0μMIncubationTime:1hourResult:InhibitedFAKTyr-397phosphorylation(pY397)andresultedinelevatedlevelsoftotalFAKprotein.體內(nèi)研究PND-1186(30mg/kgor100mg/kg;subcutaneously;injectedsubcutaneouslyintheneckregion)inhibits4T1subcutaneoustumorgrowthbyinductionofapoptosis[1].AnimalModel:BALB/cmice[1]Dosage:30mg/kgor100mg/kgAdministration:Injected(100μL)subcutaneouslyintheneckregion;every12h(twice-daily,b.i.d.)for5days.Result:100mg/kgtreatmentsignificantlyreducedfinal4T1tumorweight2-foldwhereas30mg/kgtreatmentslightlyreducedfinaltumorweightbutwasnotsignificantlydifferentcomparedtocontrol.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CancerCell.2019Mar18;35(3):457-472.e5.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?ClinCancerRes.2019Jul15;25(14):4552-4566.?bioRxiv.2020Apr.?HarvardMedicalSchoolLINCSLIBRARYSeemorecustomervalidationsonwww.MedChemEREFERENCES[1].TanjoniI,etal.PND-1186FAKinhibitorselectivelypromotestumorcellapoptosisinthree-dimensionalenvironments.CancerBiolTher.2010May15;9(10):764-77.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo