PI3Kα-IN-4-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPI3Kα-IN-4Cat.No.:HY-131345CASNo.:2322293-83-2分?式:C??H??ClFN?O?S分?量:560作?靶點(diǎn):PI3K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:100mg/mL(178.57mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7857mL8.9286mL17.8571mL5mM0.3571mL1.7857mL3.5714mL10mM0.1786mL0.8929mL1.7857mL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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.46mM);Clearsolution1/2MasterofBioactiveMolecules—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(4.46mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.46mM);ClearsolutionBIOLOGICALACTIVITY?物活性PI3Kα-IN-4?種有效的，選擇性和具有?服活性的PI3Kα抑制劑，IC50值為1.8nM。PI3Kα-IN-4具有抗腫瘤活性。IC50&TargetPI3Kα1.8nM(IC50)體外研究PI3Kα-IN-4(compound10)inhibitsPI3Kα,β,δ,andγ,withIC50sof1.8,271.0,13.9,and13.8nM,respectivelyinkinaseassays[1].PI3Kα-IN-4inhibitsPI3Kα,β,δ,andγ,withIC50sof12.1,1393,183,and>10000nM,respectivelyincellbasedassays[1].體內(nèi)研究PI3Kα-IN-4(compound10)(30mg/kg;p.o.oncedailyfor21d)achievesthebestefficacy,whichcouldinhibittumorgrowthby73.0%inmice[1].PI3Kα-IN-4(15-40mg/kg;p.o.oncedailyfor30d)dosedependentlysuppressestumorgrowthby62.5%(15mg/kg),86.0%(30mg/kg)and90.7%(40mg/kg),respectivelyinmice[1].PI3Kα-IN-4(15-40mg/kg;p.o.oncedaily;1-4h)inhibitsthephosphorylationofAktinadose-andtime-dependentmannerinvivo[1].PI3Kα-IN-4showshighCmax(mouse22167,rat2327nM)andgoodbioavailability(mouse59.4%,rat46.9%)followingoraladministration(mouse10,rat3mg/kg)[1].PI3Kα-IN-4showst1/2(mouse0.99,rat1.22h)andlowplasmaclearance(mouse4.16,rat5.28mL/min/kg)followingintravenousinjection(mouse1,rat1mg/kg)[1].AnimalModel:BT-474subcutaneousxenograftmice[1]Dosage:30mg/kgAdministration:P.o.oncedailyfor21daysResult:Inhibitedtumorgrowthby73.0%andcouldbetolerated.REFERENCES[1].DongJ,et,al.Discoveryof3-Quinazolin-4(3H)-on-3-yl-2,N-dimethylpropanamidesasOrallyActiveandSelectivePI3KαInhibitors.ACSMedChemLett.2020Jun10;11(7):1463-1469.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapp