ProductDescription
NVP-BGT226isanovelorallybioavailabledualPI3K/mTORinhibitor.ItselectivelyinhibitsPI3KandbothmTORcomplexesmTORC1andmTORC2,resultinginnearlycompletephosphorylation-inhibitionofP70S6and4E-BP1.
BGT226demonstratedexcellentcellularactivitiesininhibitingproliferations(IC50:7-30nM)ofmanytestedcelllines.Notably,cellsthatexpressPIK3CAmutationH1047Rarestillsensitivetothegrowth-inhibitionofBGT226.FlowcytometricanalysisshowsaccumulationofcellsintheG0-G1phasewithconcomitantlossintheS-phase.BGT226inducesapoptosisorautophagyofsomecancercellsatIC50lessthan25nM.Inanimalmodels,BGT226significantlydelays/inhibitstumorgrowthinadose-dependentmanner.BGT-226representsapotentialcandidateforcancertherapy.IthasenteredphaseI/IIclinicaltrialsfortreatmentofadvancedsolidtumors(includingbreastcancer)[1-4].
Technicalinformation:
| ChemicalFormula: | C28H25F3N6O2.C4H4O4 | |
| CAS#: | 1245537-68-1 | |
| MolecularWeight: | 650.6 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | 8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-oneMaleicacid | |
| Solubility: | Upto22mMinDMSO | |
| Synonyms: | NVP-BGT226,BGT226 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | BaduraS,etal.PosterAbstracts.DifferentialSuppressiveEffectsofSelectivePI3KandmTORandDualPI3K/mTORC1/C2InhibitiononLong-TermCulturedPrimaryHumanAcuteLymphoblasticLeukemia(ALL)CellsImplicateaDistinctRoleofmTORC2https://ash.confex.com/ash/2010/webprogram/Paper33127.html |
| 2. | ChangKY,etal.Novelphosphoinositide3-kinase/mTORdualinhibitor,NVP-BGT226,displayspotentgrowth-inhibitoryactivityagainsthumanheadandneckcancercellsinvitroandinvivo.ClinCancerRes.2011.17(22):7116-26.PubmedID:21976531 |
| 3. | BaumannP,etal.SimultaneoustargetingofPI3KandmTORwithNVP-BGT226ishighlyeffectiveinmultiplemyeloma.AnticancerDrugs.2012.23(1):131-8.PubmedID:21959532 |
| 4. | http://clinicaltrials.gov/ct2/show/NCT00600275 |
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