Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENSC-70220Cat.No.:HY-101796CASNo.:4551-00-2分?式:C??H??NO?分?量:325.36作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:Powder-20°C3years4°C2years*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:12.5mg/mL(38.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0735mL15.3676mL30.7352mL5mM0.6147mL3.0735mL6.1470mL10mM0.3074mL1.5368mL3.0735mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.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%salineSolubility:≥1.25mg/mL(3.84mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(3.84mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性NSC-70220?種選擇性的變構(gòu)SOS1抑制劑。NSC-70220抑制變構(gòu)位點(diǎn)激活，并部分抑制催化位點(diǎn)激活。NSC-70220具有抗癌作?。IC50&TargetSOS1[1].體外研究Thegrowthinhibitoryrate(IR)=(averageODvalueinthecontrolgroup-averageODvalueinthetreatmentgroup)/averageODvalueinthecontrolgroup×100%arecompared.TreatmentswithNSC-70220at40μMandNSC-658497at30μMresultingrowthinhibitoryrateof29%and8%respectively.Thecombinationtreatmentresultsingrowthinhibitoryrateof54%,showingthesynergisticeffectofNSC-70220andNSC-658497oncellgrowthinhibition.ItisshowedthatthetreatmentwithNSC-658497at40μMfor2hoursaloneorincombìnationwiththetreatmentwith40μMofNSC-70220overnightresultedinlowerexpressionlevelsofP-AKTandP-ERK.Thetreatmentwlth40μMofNSC-70220overnightresultedinlowerexpressionlevelsofP-ERK[1].PROTOCOLCellAssay[1]MIApaca-2cells(KRASG12C)aresubjectedtoa3-dayproliferationassayfollowingtreatmentwithSOS1-IN-1(NSC-70220:40μM),treatmentwithNSC-658497(30μM)andtreatmentwithacombinationofSOS1-IN-1(40μM)andNSC-658497(30μM).DMSOisusedasthenegativecontrol[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].ARYLSULFONOHYDRAZIDES.WO2016077793A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu