PD-184352isananticancerchemotherapeuticMEK1/2andRafinhibitorthatisparticularlyeffectiveagainstcancersharboringB-RaforRASmutationssuchasV600E.PD-184352enhancesp53accumulationandcaspaseactivation,increaseslevelsofpro-apoptoticBimprotein,anddecreasinglevelsofcyclinD1,inducingcellcyclearrestandapoptosisinseveralcancercelllines.Thiscompoundalsoinducestumorregressioninanimalmodelscarryinglungtumors.
| CasNo. | 212631-79-3 |
|---|---|
| Purity | ≥98% |
| Formula | C17H14ClF2IN2O2 |
| FormulaWt. | 478.66 |
| ChemicalName | 2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-benzamide |
| IUPACName | 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide |
| Synonym | CI-1040 |
| Solubility | SolubleinDMSO |
| Appearance | Whitetooffwhitepowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | P1200InfoSheetPDF |
|---|---|
| Brochures | Ras-Raf-MEK-ERKPathwayBooklet |
WickendenJA,JinH,JohnsonM,etal.ColorectalcancercellswiththeBRAF(V600E)mutationareaddictedtotheERK1/2pathwayforgrowthfactor-independentsurvivalandrepressionofBIM.Oncogene.2008Dec4;27(57):7150-61.PMID:18806830.
LunghiP,GiulianiN,MazzeraL,etal.TargetingMEK/MAPKsignaltransductionmodulepotentiatesATO-inducedapoptosisinmultiplemyelomacellsthroughmultiplesignalingpathways.Blood.2008Sep15;112(6):2450-62.PMID:18583568.
BainJ,PlaterL,ElliottM,etal.Theselectivityofproteinkinaseinhibitors:afurtherupdate.BiochemJ.2007Dec15;408(3):297-315.PMID:17850214.
JiH,WangZ,PereraSA,etal.MutationsinBRAFandKRASconvergeonactivationofthemitogen-activatedproteinkinasepathwayinlungcancermousemodels.CancerRes.2007May15;67(10):4933-9.PMID:17510423.
SquiresMS,NixonPM,CookSJ.Cell-cyclearrestbyPD184352requiresinhibitionofextracellularsignal-regulatedkinases(ERK)1/2butnotERK5/BMK1.BiochemJ.2002Sep1;366(Pt2):673-80.PMID:12069688.
