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| 货号： | IMA1005-0005MG |
| 保存条件： | -20 |
| CAS号： | 391210-10-9 |
| 供应商： | 上海伟进生物科技有限公司 |
| 英文名： | PD0325901(MEK1/2inhibitor) |
| 规格： | 5mg/10mg/25mg |
BiologicalActivity ........................................................................................................................................................................................................................................... PD0325901isaselective,nonATP-competitiveandhighlypotentinhibitorofmitogen-activatedproteinkinasekinase(MAPKKorMEK),withKivaluearound1nMagainstactivatedMEK1andMEK2.AsananalogofCI-1040(PD184352),PD0325901isnotonlyabout500-foldmorepotentthanCI-1040againstthephosphorylationofERK1andERK2invitrocellcultures,butshowshigherpotencyofanticanceractivityinvivo.PD0325901isgreatlyimprovedinseveralbeneficialpharmacological factors,includinglongerdurationandgreaterpotencyofMEK inhibition,aswellasgreatersolubilityleadingtoimproved bioavailability,andincreasedmetabolicstability [1-2].PD0325901potentlyinhibitstheproliferationofthyroidcancercells(IC50 =0.059-0.783μM)andarrestscellcycleattheG0/G1phaseofcellsharboringBRAForRASmutationsbutnotcellsharboringwild-typeallelesortheRET/PTC1rearrangement [3].PD0325901exertspotentgrowth-inhibitory,proapoptotic,andantiangiogenicactivitybothinvitroandinvivoxenograftmodelsofmalignantmelanoma,regardlessoftheirBRAFmutationstatus [4].PD0325901,whenconcurrentwithGSK-3βinhibitorCHIR99021preventcelldifferentiationandsustainmESCsself-renewal [5].IncombinationwithALK5inhibitorSB431542,PD0325901alsoimprovestheefficiencyofthereprogrammingprocessfromhumanfibroblasts [6].
ChemicalProperties .........................................................................................................................................................................................................................................
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