企业QQ
官方微信
MedKooCat#:201841
Name:MGCD-265-analog
CAS#:875337-44-3
ChemicalFormula:C26H20FN5O2S2
ExactMass:517.10424
MolecularWeight:517.6
ElementalAnalysis:C,60.33;H,3.89;F,3.67;N,13.53;O,6.18;S,12.39
Synonym:MGCD-265-analog;MGCD265-analog;MGCD265-analog.Glesatinib-analog.
IUPAC/ChemicalName:N-((3-fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-phenylacetamide
InChiKey:UFICVEHDQUKCEA-UHFFFAOYSA-N
InChiCode:InChI=1S/C26H20FN5O2S2/c1-32-14-20(29-15-32)23-13-19-25(36-23)22(9-10-28-19)34-21-8-7-17(12-18(21)27)30-26(35)31-24(33)11-16-5-3-2-4-6-16/h2-10,12-15H,11H2,1H3,(H2,30,31,33,35)
SMILESCode:O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=CN(C)C=N4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=CC=C5
MGCD265isanoveltargetedcancertherapeuticdiscoveredbyMethylGenethatinhibitstheMetandVEGFreceptortyrosinekinases.TheabnormalactivationofMetisinvolvedintumordevelopment,metastasisandsurvivalandtheVEGFkinaseisresponsIBLefortheinappropriateformationofbloodvessels(angiogenesis)thatnourishthetumor.Inpreclinicalstudies,MGCD265demonstratednanomolarpotencyinenzymeandcellularassaysandupto100%oftumorgrowthinhibitioninabroadrangeofxenograftmodels.
DevelopmentStatusofMGCD265:IntheongoingPhase1program,MGCD265isbeingadmiNISTeredorallyinpatientswithadvancedcancers.Thecompoundhasdemonstratedafavorablesafetyprofileandcanbecombinedsafelywithothercancertherapeuticssuchasdocetaxel(Taxotere®)anderlotinib(Tarceva®).ThesetherapeuticswereselectedforcombinationstudiesbasedonpreclinicaldatathatdemonstratedthecombinationofMGCD265anderlotinibandofMGCD265anddocetaxelshowedgreateranti-tumoractivitycomparedtoeachdrugadministeredalone.Todate,theCompanyhasinitiatedthreeclinicalstudies.(source:http://methylgene.com,accesseddate:2/1/2012)
J.M.Besterman,M.Fournel,I.Dupont,C.Bonfils,M.Dubay,H.Ste-Croix,C.R.Maroun;MethylGene,Inc.,Montreal,QC,Canada,PotentpreclinicalantitumoractivityofMGCD265,anoralMet/VEGFRkinaseinhibitorinphaseIIclinicaldevelopment,incombinationwithtaxanesorerlotinib,JClinOncol28,2010(suppl;abstre13595).
SouthernBiotech/Goat Anti-Human Lambda-Alexa Fluor® 555/2070-32/1.0 mg
vectorlabs/Biotinylated Aleuria Aurantia Lectin (AAL)/B-1395/1 mg
vectorlabs/VECTASTAIN® Elite® ABC-HRP Kit (Peroxidase, Mouse IgG)/PK-6102/1 kit
vectorlabs/VECTASTAIN® Elite® ABC-HRP Kit (Peroxidase, Universal)/PK-6200/1 kit
vectorlabs/Unconjugated Musa Paradisiaca (Banana) Lectin (BanLec)/L-1410/5 mg
GiottoBiotech/Calmodulin N60D/5 mg/G02CLM60cn