PND-1186-VS-4718-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPND-1186Cat.No.:HY-13917CASNo.:1061353-68-1Synonyms:VS-4718;SR-2516分?式:C??H??F?N?O?分?量:501.5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:≥34mg/mL(67.80mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9940mL9.9701mL19.9402mL5mM0.3988mL1.9940mL3.9880mL10mM0.1994mL0.9970mL1.9940mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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:≥2.5mg/mL(4.99mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.99mM);Clearsolution3.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.99mM);ClearsolutionBIOLOGICALACTIVITY?物活性PND-1186(VS-4718)?種有效的，?特異性的，可逆的FAK抑制劑，IC50為1.5nM。PND-1186選擇性促進腫瘤細胞凋亡(apoptosis)[1]。IC50&TargetIC50:1.5nM(FAK)[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.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻?CancerCell.2019Mar18;35(3):457-472.e5.?ClinCancerRes.2019Jul15;25(14):4552-4566.?JExpClinCancerRes.2022Jun3;41(1):193.?bioRxiv.2020Apr.?HarvardMedicalSchoolLINCSLIBRARYSeemorecustomervalidationsonwww.MedChemEREFERENCES[1].TanjoniI,etal.PND-1186FAKinhibitorselectivelypromotestumorcellapoptosisinthree-dimensionalenvironments.CancerBiolTher.2010May15;9(10):764-77.McePdfHeightCaution:Producthasnotbeenfullyvalidate