Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETASP0415914Cat.No.:HY-120438CASNo.:1292300-75-4分?式:C??H??N?O?S分?量:323.37作?靶點:PI3K;Akt作?通路:PI3K/Akt/mTOR儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:125mg/mL(386.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0924mL15.4622mL30.9243mL5mM0.6185mL3.0924mL6.1849mL10mM0.3092mL1.5462mL3.0924mL請根據產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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.43mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.43mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性TASP0415914?種有效且具有?服活性的PI3Kγ抑制劑，IC50為29nM。TASP0415914還顯?出有效的Akt抑制活性，IC50為294nM。TASP0415914可?于炎癥性疾病的研究。IC50&TargetPI3KγAkt29nM(IC50)294nM(IC50)體外研究TASP0415914(compound8j)showshighmetabolicstabilityinrat/humanlivermicrosomes.TASP0415914hasnoCYPinhibitionupto10μMforCYP1A2,2C9,2C19,2D6and3A4[1].體內研究TASP0415914(compound8j;10-100mg/kg;orallyadministration;twicedaily;for14days)treatmentsuppressedtheprogressionofthediseaseinadose-dependentmannerinamousecollagen-inducedarthritis(CIA)model[1].AnimalModel:Collagen-primedDBA/1mice[1]Dosage:10mg/kg;30mg/kg;100mg/kgAdministration:Orallyadministration;twicedaily;for14daysResult:Suppressedtheprogressionofthediseaseinadose-dependentmanner.REFERENCES[1].YusukeOka,etal.DiscoveryofN-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide(TASP0415914)asanorallypotentphosphoinositide3-kinaseγinhibitorforthetreatmentofinflammatorydiseases.BioorgMedChem.2013Dec15;21(24):7578-83.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu