Cellagentech/BIBW2992(阿法替尼)| EGFR,Her2抑制剂/C2929-5/5 mg(粉末)

价格
¥2380.00
货号:C2929-5
浏览量:127
品牌:Cellagen
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ProductDescription

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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