CC-90005-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECC-90005Cat.No.:HY-132304CASNo.:1799574-70-1分?式:C??H??F?N?O?分?量:447.48作?靶點:PKC作?通路:Epigenetics;TGF-beta/Smad儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:62.5mg/mL(139.67mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2347mL11.1737mL22.3474mL5mM0.4469mL2.2347mL4.4695mL10mM0.2235mL1.1174mL2.2347mL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(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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.25mg/mL(2.79mM);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:≥1.25mg/mL(2.79mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(2.79mM);ClearsolutionBIOLOGICALACTIVITY?物活性CC-90005?種有效，選擇性和具有?服活性的蛋?激酶C-θ(PKC-θ)抑制劑，IC50值為8nM。CC-90005顯?了對PKC-θ的選擇性超過PKC-δ(IC50=4440nM)。CC-90005可以通過IL-2表達抑制T細胞活化。IC50&TargetPKCθ8nM(IC50)體外研究CC-90005showstheexquisiteselectivityofCC-90005,withIC50sforallotherfamilymembersof>3μM[1].CC-90005isamoderateinhibitorofbothCYP2C9(IC50=8μM)andCYP2C19(IC50=5.9μM)inhumanlivermicrosomes[1].CC-90005inhibitsIL-2expressioninLRS_WBChumanPBMCs,withanIC50of0.15μM[1].CC-90005(1-10μM;24h)inhibitsTcellproliferationinPBMCsby51%at1μMand88%at3μM[1].體內研究CC-90005(3-30mg/kg;p.o.twicedailyfor4days)significantlyreducesthepopliteallymphnode(PLN)sizeinamodelofchronicTcellactivation[1].CC-90005(100mg/kg;asinglep.o.)significantlyinhibitsplasmaandspleenIL-2releaseby51and54%,respectively[1].CC-90005exhibitsreasonableoralbioavailability(66and46%)andCmax(1.18and1.2μM)followingoraladministration(10and3mg/kg)inratanddog,respectively[1].CC-90005exhibitsthemeanresidencetime(0.52and2.0h),CL(69.1and20.5mL/min/kg)andVss(2.11and2.44L/kg)followingintravenousadministration(2and1mg/kg)inratanddog,respectively[1].AnimalModel:B6D2F1mice(20g)wereinjectedwithallogeneicspleencellsDosage:3,10,30mg/kgAdministration:P.o.twicedailyfor4daysResult:InhibitedPLNsizeby45and38%atdosesof10and30mg/kg,respectively.REFERENCES[1].PapaP,et,al.DiscoveryoftheSelectiveProteinKinaseC-θKinaseInhibitor,CC-90005.JMedChem.2021Aug26;64(16):11886-11903.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala