Description
DCC-2036(rebastinib)isanAblinhibitorthatexhibitsanticanceractivity.Incellularmodelsofchronicmyelogenousleukemia(CML),rebastinibinducesapoptosisandinhibitscellproliferation.RebastinibbindstheswitchcontrolpocketofAblthatisinvolvedinconformationalregulationofthekinasedomain.
References
ShenY,ShiX,PanJ.TheconformationalcontrolinhibitoroftyrosinekinasesDCC-2036iseffectiveforimatinib-resistantcellsexpressingT674IFIP1L1-PDGFRα.PLoSOne.2013Aug29;8(8):e73059.PMID:24009732.
EideCA,AdrianLT,TynerJW,etal.TheABLswitchcontrolinhibitorDCC-2036isactiveagainstthechronicmyeloidleukemiamutantBCR-ABLT315Iandexhibitsanarrowresistanceprofile.CancerRes.2011May1;71(9):3189-95.PMID:21505103.