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BKM120isapotentandhighlyspecificpan-classIPI3Kinhibitor.Itexhibits50-300nMactivityforclassIPI3Ks,includingthemostcommonp110?mutants.ItislesspotentagainstclassIIIandclassIVPI3Ks.Inaddition,itshowsnosignificantinhibitionagainstrelatedkinases,includingVPS34,mTOR,DNAPKandPI4K[1].
AbnormalactivationofthePI3K-AKT-mTORpathwayisfrequentlyobservedinmanytypesofcancer.TargetingthePI3K-AKT-mTORpathwaycouldarresttumorgrowthandinducecelldeathincancers.KM120aloneorincombinationwithotheragentsinducedapoptosisandinhibitproliferation(IC50of0.15-0.7nM)inabroadrangeofPI3Kderegulatedtumorcells.InhibitionofPI3KbyBMK120togetherwithSTAT3blockadeinducesapoptosissynergisticallyingastriccancercellsharboringmutatedKRASbutnotinKRASwild-typecells.BKM120treatmentresultsinsignificantlyreducedtumorvolumeandprolongedsurvivalinmousemodels[1-4].BKM120iscurrentlybeinginvestigatedinPhaseIandIIclinicaltrialsinadvancedsolidtumorpatientsasasingleagentaswellasincombinationwithotheragents.
Technicalinformation:
| ChemicalFormula: | C18H21F3N6O2 | |
| CAS#: | 944396-07-0 | |
| MolecularWeight: | 410.39 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | NVP-BKM120,BKM120 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Burger,MT,etalIdentificationofNVP-BKM120asaPotent,Selective,OrallyBioavailableClassIPI3KinaseInhibitorforTreatingCancer.ACSMed.Chem.Lett.,2011,2(10),pp774779. |
| 2. | KoulD,etel.AntitumoractivityofNVP-BKM120--aselectivepanclassIPI3kinaseinhibitorshoweddifferentialformsofcelldeathbasedonp53statusofgliomacells.ClinCancerRes.2012.18(1):184-95.PubmedID:22065080 |
| 3. | ZhengY,etal.Novelphosphatidylinositol3-kinaseinhibitorNVP-BKM120inducesapoptosisinmyelomacellsandshowssynergisticanti-myelomaactivitywithdexamethasone.JMolMed(Berl).2012.90(6):695-706.PubmedID:22207485 |
| 4. | ParkE,etal.NVP-BKM120,anovelPI3Kinhibitor,showssynergismwithaSTAT3inhibitorinhumangastriccancercellsharboringKRASmutations.IntJOncol.2012.40(4):1259-66.PubmedID:22065080 |
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