MedKoo Biosciences/KCN1/401515/100mg

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货号:401515-100mg
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品牌:MedKoo
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商品描述
KCN1,anovelsyntheticsulfonamide,isaHIFpathwayinhibitorwithpotentialanticanceractivityinvitroandinvivoanti-pancreaticcanceractivitiesandpreclinicalpharmacology.KCN1specificallyinhibitedHIFreportergeneactivityinseveralgliomacelllinesatthenanomolarlevel.KCN1alsodownregulatedtranscriptionofendogenousHIF-1targetgenes,suchasVEGF,Glut-1,andcarbonicanhydrase9,inahypoxia-responsiveelement(HRE)-dependentmanner.KCN1potentlyinhibitedthegrowthofsubcutaneousmalignantgliomatumorxenograftswithminimaladverseeffectsonthehost.MechaNISTically,KCN1didnotdownregulatethelevelsofHIF-1αorothercomponentsoftheHIFtranscriptionalcomplex;rather,itantagonizedhypoxia-inducIBLetranscriptionbydisruptingtheinteractionofHIF-1αwithtranscriptionalcoactivatorsp300/CBP.CONCLUSIONS:ThenewHIFpathwayinhibitorKCN1hasantitumoractivityinmousemodels,supportingitsfurthertranslationforthetreatmentofhumantumorsdisplayinghypoxiaorHIFoverexpression(source:ClinCancerRes.2012Nov21.[Epubaheadofprint])

MedKooCat#:401515
Name:KCN1
CAS#:927823-01-6
ChemicalFormula:C26H27NO5S
ExactMass:465.16099
MolecularWeight:465.56
ElementalAnalysis:C,67.08;H,5.85;N,3.01;O,17.18;S,6.89


Synonym:KCN1;KCN-1;KCN1.

IUPAC/ChemicalName:3,4-dimethoxy-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]-N-phenylbenzenesulfonamide

InChiKey:IPZJNJPAVPZHJM-UHFFFAOYSA-N

InChiCode:InChI=1S/C26H27NO5S/c1-26(2)15-14-20-16-19(10-12-23(20)32-26)18-27(21-8-6-5-7-9-21)33(28,29)22-11-13-24(30-3)25(17-22)31-4/h5-17H,18H2,1-4H3

SMILESCode:O=S(C1=CC=C(OC)C(OC)=C1)(N(CC2=CC(C=CC(C)(C)O3)=C3C=C2)C4=CC=CC=C4)=O


TechnicalData

Appearance:
Solidpowder

Purity:
>98%

ShippingCondition:
Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

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

Solubility:
SolubleinDMSO,notinwater

ShelfLife:
>5yearsifstoredproperly

DrugFormulation:
ThisdrugmaybeformulatedinDMSO

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

HarmonizedSystemCode:
293490


AdditionalInformation

   
ThefollowingdatawasfromPLoSOne.2012;7(9):e44883.doi:10.1371/journal.pone.0044883.Epub2012Sep13.
   
  
  
Figure1.InvitroanticanceractivitiesofKCN1againstpancreaticcancercells. (B)CellgrowthinhibitoryactivityofKCN1inhumanpancreaticcancercells.CellswereexposedtovariousconcentrationsofKCN1for72h,followedbyanMTTassay.(Source:PLoSOne.2012;7(9):e44883.doi:10.1371/journal.pone.0044883.Epub2012Sep13.)
Figure1.InvitroanticanceractivitiesofKCN1againstpancreaticcancercells. (B)CellgrowthinhibitoryactivityofKCN1inhumanpancreaticcancercells.CellswereexposedtovariousconcentrationsofKCN1for72h,followedbyanMTTassay.(
)
   
   
     
     


References

1:WangW,AoL,RayburnER,XuH,ZhangX,ZhangX,NagSA,WuX,WangMH,WangH,VanMeirEG,ZhangR.KCN1,anovelsyntheticsulfonamideanticanceragent:invitroandinvivoanti-pancreaticcanceractivitiesandpreclinicalpharmacology.PLoSOne.2012;7(9):e44883.doi:10.1371/journal.pone.0044883.Epub2012Sep13.PubMedPMID:23028659;PubMedCentralPMCID:PMC3441526.

2:YinS,KaluzS,DeviNS,JabbarAA,deNoronhaRG,MunJ,ZhangZ,BoreddyPR,WangW,WangZ,AbbruscatoT,ChenZ,OlsonJJ,ZhangR,GoodmanMM,NicolaouKC,VanMeirEG.ArylsulfonamideKCN1InhibitsInVivoGliomaGrowthandInterfereswithHIFSignalingbyDisruptingHIF-1αInteractionwithCofactorsp300/CBP.ClinCancerRes.2012Nov21.[Epubaheadofprint]PubMedPMID:22923450;PubMedCentralPMCID:PMC3518680.
 
  

苏州蚂蚁淘代理MedKoo在中国的业务。 MedKoo北京代理,MedKoo华东代理,MedKoo华北代理,MedKoo华中代理,MedKoo华南代理,MedKoo全国代理。 MedKoo公司是2009年由Qingqi Chen博士创立。在美国北卡罗来纳州的三角研究园区有运营办公室,其研发和生产车间位于中国。陈博士在加入MedKoo之前,是中山大学药学院(中山大学,中国广州)和中国科学院(北京)“100人计划”的杰出教授。对小分子抗癌药物有浓厚兴趣,发表了100多篇论文,获得20多项。Medkoo是处于先进地位的小分子抗癌试剂,激酶抑制剂和其他相关化学品的优秀供应商。 MedKoo部分产品列表:MedKoo全国代理 406757 10058-F4 530576 10074-G5 600110 10-Deacetylbaccatin III 530429 10-Gingerol 406281 10-Hydroxycamptothecin 341231 10-Hydroxyyohimbine 571387 [11C]-ABP688 526406 11-deoxy-PGF2a 525629 123C4   561223 12-Crown-4 featured 525697 1,3,5,6-Tetrahydroxyxanthone 526087 1,3,5-Trihydroxyxanthone 584120 1,3,7-Trimethyluric acid 527871 1,3-Dicaffeoylquinic acid 530605 1400W HCl