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BIBW2992(Afatinib)isanorally-available,aminoquinazoline-acrylamide-basedinhibitorwithIC50potencyforEGFRwt,EGFR(L858R),EGFR(L858R/T790M),andHER2at0.5,0.4,10,and14nM,respectively.[1]Viaitscrotonamidefunctionalgroup,BIBW2992targetstheErbBfamilyinanirreversIBLemanner,providingasustained,selective,andcovalentinhibitionthathasbeenshowntobeeffectivetowarderlotinib-resistanttumors.[2]
Incellularassays,BIBW2992inhibitsphosphorylationofEGFRwildtype(A431),EGFR(NCI-H1975),andHER2(BT474)atEC50sof8,49,and75nM,respectively.[3]
BIBW2992displayspotentgrowthinhibitionofEGFR/HER2expressinglungcancercelllinesH1666,H3255,andNCI1975atIC50valuesof60,0.7,and99nM,respectively.[1]
Technicalinformation:
| ChemicalFormula: | C24H25ClFN5O3 | |
| CAS#: | 439081-18-2 | |
| MolecularWeight: | 485.94 | |
| Purity: | >98% | |
| Appearance: | OffWhite | |
| ChemicalName: | (S,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | BIBW2992,BIBW-2992,Afatinib,Tovok,Tomtovok |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Lietal.,BIBW2992,anirreversibleEGFR/HER2inhibitorhighlyeffectiveinpreclinicallungcancermodels.Oncogene,2008,27(34),4702-4711.PubmedID:18408761 |
| 2. | BoehringerIngelheimbackgrounder(BIBW2992,Afatinib),May,2012. |
| 3. | Solcaetal.,Targetbindingpropertiesandcellularactivityofafatinib(BIBW2992),anirreversibleErbBfamilyblocker.J.Pharmacol.Exp.Ther.2012,343(2),342-350.PubmedID:22888144 |
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