MedKoo Biosciences/FIIN2/406652/200mg

FIIN-2isapotent,selective,irreversIBLeandthenext-generationcovalentFGFRinhibitor.FIIN-2isthefirstinhibitorthatcanpotentlyinhibittheproliferationofcellsdependentuponthegatekeepermutantsofFGFR1orFGFR2,whichconferresistancetofirst-generationclinicalFGFRinhibitorssuchasNVP-BGJ398andAZD4547.FIIN-2alsobindsintheDFG-outmodedespitelackingafunctionalgroupnecessarytooccupythepocketvacatedupontheDFG-outflip.

MedKooCat#:406652
Name:FIIN-2
CAS#:1633044-56-0
ChemicalFormula:C35H38N8O4
ExactMass:634.3016
MolecularWeight:634.72742
ElementalAnalysis:C,66.23;H,6.03;N,17.65;O,10.08


Synonym:FIIN2;FIIN2;FIIN-2.

IUPAC/ChemicalName:N-(4-((3-(3,5-dimethoxyphenyl)-7-((4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide

InChiKey:DVBPRWJMHURKHP-UHFFFAOYSA-N

InChiCode:InChI=1S/C35H38N8O4/c1-5-32(44)37-26-8-6-24(7-9-26)22-43-33-25(23-42(35(43)45)29-18-30(46-3)20-31(19-29)47-4)21-36-34(39-33)38-27-10-12-28(13-11-27)41-16-14-40(2)15-17-41/h5-13,18-21H,1,14-17,22-23H2,2-4H3,(H,37,44)(H,36,38,39)

SMILESCode:O=C(NC1=CC=C(C=C1)CN2C(N(CC3=CN=C(N=C32)NC4=CC=C(C=C4)N5CCN(CC5)C)C6=CC(OC)=CC(OC)=C6)=O)C=C


TechnicalData

Appearance:
Solidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

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:TanL,WangJ,TanizakiJ,HuangZ,ArefAR,RusanM,ZhuSJ,ZhangY,ErcanD,LiaoRG,CapellettiM,ZhouW,HurW,KimN,SimT,GaudetS,BarbieDA,YehJR,YunCH,HammermanPS,MohammADIM,JännePA,GrayNS.Developmentofcovalentinhibitorsthatcanovercomeresistancetofirst-generationFGFRkinaseinhibitors.ProcNatlAcadSciUSA.2014Nov11;111(45):E4869-77.doi:10.1073/pnas.1403438111.Epub2014Oct27.PubMedPMID:25349422;PubMedCentralPMCID:PMC4234547.

2:HuangZ,TanL,WangH,LiuY,BlaisS,DengJ,NeubertTA,GrayNS,LiX,MohammadiM.DFG-outmodeofinhibitionbyanirreversibletype-1inhibitorcapableofovercominggate-keepermutationsinFGFreceptors.ACSChemBiol.2015Jan16;10(1):299-309.doi:10.1021/cb500674s.Epub2014Oct27.PubMedPMID:25317566;PubMedCentralPMCID:PMC4301177.

 


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