MedKoo Biosciences/Regorafenib/202436/5g

Regorafenib,alsoknownasBAY73-4506;isanorallybioavailablesmallmoleculewithpotentialantiangiogenicandantineoplasticactivities.Regorafenibbindstoandinhibitsvascularendothelialgrowthfactorreceptors(VEGFRs)2and3,andRet,Kit,PDGFRandRafkinases,whichmayresultintheinhibitionoftumorangiogenesisandtumorcellproliferation.RegorafenibdemonstratedtoincreasetheoverallsurvivalofpatientswithmetastaticcolorectalcancerandhasbeenapprovedbytheUSFDAonSeptember27,2012.

MedKooCat#:202436
Name:Regorafenib
CAS#:755037-03-7
ChemicalFormula:C21H15ClF4N4O3
ExactMass:482.07688
MolecularWeight:482.81541
ElementalAnalysis:C,52.24;H,3.13;Cl,7.34;F,15.74;N,11.60;O,9.94

Synonym:BAY734506;BAY734506;BAY-734506;Regorafenib.tradename:Stivarga.

IUPAC/ChemicalName:4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide

InChiKey:ZFLJHSQHILSNCM-UHFFFAOYSA-N

InChiCode:InChI=1S/C21H27N7O/c1-2-4-15(5-3-1)24-20-18-19(23-14-22-18)26-21(27-20)25-16-6-8-17(9-7-16)28-10-12-29-13-11-28/h6-9,14-15H,1-5,10-13H2,(H3,22,23,24,25,26,27)

SMILESCode:C12=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC(NC5CCCCC5)=C1NC=N2

TechnicalData

Appearance:

Off-whitetolightpinksolidpowder

Purity:

>98%(orrefertotheCertificateofAnalysis)

CertificateofAnalysis:

ViewCoA,previousbatch,Lot#CT40403
ViewCoA:previousbatch,Lot#BBC40903
ViewCoA:currentbatch,Lot#TZC50818

QCData:

ViewQCdata,previousbatch,Lot#BBC40903
ViewQCdata:currentbatch,Lot#TZC50818

SafetyDataSheet(MSDS):

ViewMaterialSafetyDataSheet(MSDS)

ShippingCondition:

Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:

Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:

SolubleinDMSO,notinwater

ShelfLife:

>2yearsifstoredproperly

DrugFormulation:

ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:

0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:

293490

AdditionalInformation

References

1:RaviS,SingalAK.Regorafenib:anevidence-basedreviewofitspotentialinpatientswithadvancedlivercancer.CoreEvid.2014Jul17;9:81-7.doi:10.2147/CE.S48626.eCollection2014.Review.PubMedPMID:25114628;PubMedCentralPMCID:PMC4109634.

2:Abdel-RahmanO,FouadM.Riskofcardiovasculartoxicitiesinpatientswithsolidtumorstreatedwithsunitinib,axitinib,cediraniborregorafenib:Anupdatedsystematicreviewandcomparativemeta-analysis.CritRevOncolHematol.2014Jul1.pii:S1040-8428(14)00114-0.doi:10.1016/j.critrevonc.2014.06.003.[Epubaheadofprint]Review.PubMedPMID:25028151.

3:KhanG,MossRA,BraitehF,SaltzmanM.Proactivestrategiesforregorafenibinmetastaticcolorectalcancer:implicationsforoptimalpatientmanagement.CancerManagRes.2014Mar4;6:93-103.doi:10.2147/CMAR.S52217.eCollection2014.Review.PubMedPMID:24623990;PubMedCentralPMCID:PMC3949557.

4:DeWitM,Boers-DoetsCB,SaettiniA,VermeerschK,deJuanCR,OuwerkerkJ,RaynardSS,BazinA,CremoliniC.Preventionandmanagementofadverseeventsrelatedtoregorafenib.SupportCareCancer.2014Mar;22(3):837-46.doi:10.1007/s00520-013-2085-z.Epub2013Dec14.Review.PubMedPMID:24337717;PubMedCentralPMCID:PMC3913844.

5:Lyseng-WilliamsonKA.Regorafenib:aguidetoitsuseinadvancedgastrointestinalstromaltumor(GIST)afterfailureofimatinibandsunitinib.BioDrugs.2013Oct;27(5):525-31.doi:10.1007/s40259-013-0061-2.Review.PubMedPMID:23975637.

6:Regorafenib(Stivarga)formetastaticcolorectalcancerandGIST.MedLettDrugsTher.2013Apr29;55(1415):e36.Review.PubMedPMID:23836345.

7:SirohiB,PhilipDS,ShrikhandeSV.Regorafenib:carvinganicheinthecrowdedtherapeuticlandscape.ExpertRevAnticancerTher.2013Apr;13(4):385-93.doi:10.1586/era.13.12.Review.PubMedPMID:23560833.

8:DavisSL,EckhardtSG,MessersmithWA,JimenoA.Thedevelopmentofregorafenibanditscurrentandpotentialfutureroleincancertherapy.DrugsToday(Barc).2013Feb;49(2):105-15.doi:10.1358/dot.2013.49.2.1930525.Review.PubMedPMID:23462625.

9:RomanD,WhitesideR.Regorafenib:AddingtotheArmamentariumforRefractoryColorectalCancerandGIST.JAdvPractOncol.2013Mar;4(2):118-22.Review.PubMedPMID:25031991;PubMedCentralPMCID:PMC4093419.

10:AprileG,MacerelliM,GiulianiF.Regorafenibforgastrointestinalmalignancies:frompreclinicaldatatoclinicalresultsofanovelmulti-targetinhibitor.BioDrugs.2013Jun;27(3):213-24.doi:10.1007/s40259-013-0014-9.Review.PubMedPMID:23435872.

11:StrumbergD,SchultheisB.Regorafenibforcancer.ExpertOpinInvestigDrugs.2012Jun;21(6):879-89.doi:10.1517/13543784.2012.684752.Review.PubMedPMID:22577890.

对照品标准品，生物试剂盒，gibco胎牛血清，试剂采购网，中国试剂网，细胞因子试剂盒

MedKoo Biosciences/Regorafenib/202436/5g

TechnicalData

AdditionalInformation

References