MedKoo Biosciences/BMS833923 (XL139)/200535/5mg

BMS-833923,alsoknownasXL-139,isanorallybioavailablesmall-moleculeSMO(Smoothened)inhibitorwithpotentialantineoplasticactivity.SMOantagonistBMS-833923inhibitsthesonichedgehog(SHH)pathwayproteinSMO,whichmayresultinasuppressionoftheSHHsignalingpathway.SMOisaG-proteincoupledreceptorthatliesjustdownstreamoftheSHHligandcellsurfacereceptorPatched-1intheSHHpathway;intheabsenceofligandPatched-1inhibitsSMOandligandbindingtoPatched-1resultsinincreasedlevelsofSMO.TheSHHsignalingpathwayplaysanimportantroleincellulargrowth,differentiationandrepair;constitutiveactivationofthispathwayisassociatedwithuncontrolledcellularproliferationandhasbeenobservedinavarietyofcancers.

MedKooCat#:200535
Name:BMS-833923(XL-139)
CAS#:1059734-66-5
ChemicalFormula:C30H27N5O
ExactMass:473.22156
MolecularWeight:473.57
ElementalAnalysis:C,76.09;H,5.75;N,14.79;O,3.38

Synonym:BMS833923;BMS-833923;BMS833923;XL139;XL-139;XL139.

IUPAC/ChemicalName:N-(2-methyl-5-((methylamino)methyl)phenyl)-4-((4-phenylquinazolin-2-yl)amino)benzamide.

InChiKey:KLRRGBHZCJLIEL-UHFFFAOYSA-N

InChiCode:InChI=1S/C30H27N5O/c1-20-12-13-21(19-31-2)18-27(20)33-29(36)23-14-16-24(17-15-23)32-30-34-26-11-7-6-10-25(26)28(35-30)22-8-4-3-5-9-22/h4-18,31H,19H2,1-2H3,(H,33,36)(H,32,34,35)

SMILESCode:O=C(NC1=CC(CNC)=CC=C1C)C2=CC=C(NC3=NC(C4=CC=CC=C4)=C5C=CC=CC5=N3)C=C2.

TechnicalData

Appearance:

whitesolidpowder

Purity:

>98%(orrefertotheCertificateofAnalysis)

CertificateofAnalysis:

ViewcurrentbatchofCoA

QCData:

ViewNMR,ViewHPLC,ViewMS

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:WilkinsonSE,FuricL,BuchananG,LarssonO,PedersenJ,FrydenbergM,RisbridgerGP,TaylorRA.Hedgehogsignalingisactiveinhumanprostatecancerstromaandregulatesproliferationanddifferentiationofadjacentepithelium.Prostate.2013Dec;73(16):1810-23.doi:10.1002/pros.22720.Epub2013Sep16.PubMedPMID:24105601.

2:ZaidiAH,KomatsuY,KellyLA,MalhotraU,RotoloniC,KosovecJE,ZahoorH,MakielskiR,BhattA,HoppoT,JobeBA.Smoothenedinhibitionleadstodecreasedproliferationandinducesapoptosisinesophagealadenocarcinomacells.CancerInvest.2013Aug;31(7):480-9.doi:10.3109/07357907.2013.820317.PubMedPMID:23915072.

3:SandhiyaS,MelvinG,KumarSS,DkharSA.Thedawnofhedgehoginhibitors:Vismodegib.JPharmacolPharmacother.2013Jan;4(1):4-7.doi:10.4103/0976-500X.107628.PubMedPMID:23662017;PubMedCentralPMCID:PMC3643342.

4:AliFR,LearJT.Systemictreatmentsforbasalcellcarcinoma(BCC):theadventofdermato-oncologyinBCC.BrJDermatol.2013Jul;169(1):53-7.doi:10.1111/bjd.12311.Review.PubMedPMID:23488543.

5:GibsonMK,ZaidiAH,DavisonJM,SanzAF,HoughB,KomatsuY,KosovecJE,BhattA,MalhotraU,FoxwellT,RotoloniCL,HoppoT,JobeBA.PreventionofBarrettesophagusandesophagealadenocarcinomabysmoothenedinhibitorinaratmodelofgastroesophagealrefluxdisease.AnnSurg.2013Jul;258(1):82-8.doi:10.1097/SLA.0b013e318270500d.PubMedPMID:23108119.

6:CortesJ,GoldmanJM,HughesT.Currentissuesinchronicmyeloidleukemia:monitoring,resistance,andfunctionalcure.JNatlComprCancNetw.2012Oct1;10Suppl3:S1-S13.PubMedPMID:23055247.

7:TangJY,MarghoobAA.Emergingtreatmentsandsignalingpathwayinhibitors.SeminCutanMedSurg.2011Dec;30(4Suppl):S14-8.doi:10.1016/j.sder.2011.11.002.Review.PubMedPMID:22177102.

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MedKoo Biosciences/BMS833923 (XL139)/200535/5mg

TechnicalData

AdditionalInformation

References