Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPQR530Cat.No.:HY-107365CASNo.:1927857-61-1分?式:C??H??F?N?O?分?量:407.42作?靶點(diǎn):PI3K;mTOR作?通路:PI3K/Akt/mTOR儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:33.33mg/mL(81.81mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4545mL12.2723mL24.5447mL5mM0.4909mL2.4545mL4.9089mL10mM0.2454mL1.2272mL2.4545mL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；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)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:2.5mg/mL(6.14mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.14mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.14mM);ClearsolutionBIOLOGICALACTIVITY?物活性PQR530?種有效，ATP競(jìng)爭(zhēng)性的，具有?服活性，可透過(guò)?腦屏障的，PI3K/mTORC1/2雙重抑制劑，對(duì)于PI3Kα和mTOR(分別為0.84和0.33nM)的Kd為亞爾。具有抗腫瘤活性。IC50&TargetmTORPI3KαPI3KβPI3Kγ0.33nM(Kd)0.84nM(Kd)6.1nM(Kd)10nM(Kd)PI3KδPI3KC2β11nM(Kd)100nM(Kd)體外研究PQR-530isapotent,oralandbrain-penetrantdualpan-PI3K/mTORC1/2inhibitor,exhibitingantitumoractivity.PQR-530inhibitsallPI3KisoformsandmTORcomplexesC1/2potentlyandselectively.PQR-530inhibitsproteinkinaseB(PKB,pSer473)andribosomalproteinS6(pS6,pSer235/236)phosphorylationwithIC50valuesof0.07μMinA2058melanomacells.PQR-530showsinhibitoryactivityagainstthegrowthof44cancercelllineswithmeanGI50of426nM[1].REFERENCES[1].DeniseRageot,etal.Abstract140:DiscoveryandbiologicalevaluationofPQR530,ahighlypotentdualpan-PI3K/mTORC1/2inhibitor.CancerRes2017;77(13Suppl).[2].RageotD,etal.(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine(PQR530),aPotent,OrallyBioavailable,andBrain-PenetrableDualInhibitorofClassIPI3KandmTORKinase.JMedChem.2019;62(13):6241-62McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc