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BAY-73-4506(Regorafenib)isanorallyactiveandhighlypotentinhibitoragainstmultipletyrosinekinases,includingVEGFR1/2/3,PDGFR?,Kit,RETandRaf-1.RegorafenibinhibitstheproliferationofHUVECcellsstimulatedwithVEGF,andinhibitsFGFRsignalinginbreastcancerMCF-7cellsstimulatedwithFGF.Regorafenibisanti-angiogenicduetoitsinhibitionsagainstVEGFR2-TIE2tyrosinekinase.[1]
Co-admiNISTrationofRegorafenibandaPI3K/Aktinhibitor(MK-2206)clearlydemonstratedsynergisticeffectinaHCT116xenocraftmousemodel[2].Regorafenibiscurrentlybeingstudiedasapotentialtreatmentoptioninmultipletumortypes,andhasrecentlybeapprovedintreatingpatientswithMetastaticColorectalcancer.[3]
Technicalinformation:
| ChemicalFormula: | C21H15ClF4N4O3 | |
| CAS#: | 755037-03-7 | |
| MolecularWeight: | 482.82 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | BAY-73-4506,BAY73-4506,Regorafenib,Fluoro-Sorafenib |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderorDMSOsolutionat-20oCdesiccated.
Reference:
| 1. | WilhelmSMetal,Regorafenib(BAY73-4506):aneworalmulti-kinaseinhibitorofangiogenic,stromalandoncogenicreceptortyrosinekinaseswithpotentpreclinicalantitumoractivity.IntJCancer.2011;129:245-55PubmedID:21170960 |
| 2. | SajithlalGBetal.Sorafenib/regorafenibandphosphatidylinositol3kinase/thymomaviralproto-oncogeneinhibitioninteracttokilltumorcells.MolPharmacol.2013;84(4):562-71.PubmedID:23877009 |
| 3. | CarterNJ.Regorafenib:areviewofitsuseinpreviouslytreatedpatientswithprogressivemetastaticcolorectalcancer.DrugsAging.2014;31(1):67-78.PubmedID:24276917 |
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