Catalog Number: 4192
Alternate Names: PD325901
Chemical Name: N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide
Biological Activity
Potent MEK1 and MEK2 inhibitor. Inhibits MEK activity in mouse colon 26 cells (IC50 = 0.33 nM). Inhibits the growth of melanoma cell lines in vitro and in vivo; induces G1-phase cell cycle arrest and apoptosis in a mouse xenograft model. Also inhibits production of proangiogenic cytokines such as VEGF. Enhances generation of induced pluripotent stem cells (iPSCs). Orally active.
Technical Data
  • M.Wt:
    482.19
  • Formula:
    C16H14F3IN2O4
  • Solubility:
    Soluble to 25 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    391210-10-9
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations.
    Ciuffreda et al.
    Neoplasia, 2009;11:720
  2. A chemical platform for improved induction of human iPSCs.
    Lin et al.
    Nat.Methods., 2009;6:805
  3. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
    Barrett et al.
    Bioorg.Med.Chem.Lett., 2008;18:6501
  4. The biological profile of PD 0325901: a second generation analog of CI-1040 with improved pharmaceutical potential.
    Sebolt-Leopold et al.
    Proc.Amer.Assoc.Cancer Res., 2004;45:925
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PD 0325901 include:

9 Citations: Showing 1 - 9
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  1. Poly(I:C) increases the expression of mPGES-1 and COX-2 in rat primary microglia.
    Authors: Oliveira Et al.
    Stem Cells 2016;13:11
  2. Transient acquisition of pluripotency during somatic cell transdifferentiation with iPSC reprogramming factors.
    Authors: Maza Et al.
    Nat Biotechnol 2015;33:769
  3. HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity.
    Authors: Mattis Et al.
    PLoS One 2015;24:3257
  4. Functional annotation of native enhancers with a Cas9-histone demethylase fusion.
    Authors: Kearns Et al.
    Nat Methods 2015;12:401
  5. The bimodally expressed microRNA miR-142 gates exit from pluripotency.
    Authors: Sladitschek and Neveu
    J Neuroinflammation 2015;11:850
  6. Manganese Superoxide Dismutase Gene Expression Is Induced by Nanog and Oct4, Essential Pluripotent Stem Cells' Transcription Factors.
    Authors: Solari Et al.
    Mol Syst Biol 2015;10:e0144336
  7. A method to identify and isolate pluripotent human stem cells and mouse epiblast stem cells using lipid body-associated retinyl ester fluorescence.
    Authors: Muthusamy Et al.
    Stem Cell Reports 2014;3:169
  8. Glycogen synthase kinase 3β and activin/nodal inhibition in human embryonic stem cells induces a pre-neuroepithelial state that is required for specification to a floor plate cell lineage.
    Authors: Denham Et al.
    Development 2012;30:2400
  9. Conversion from mouse embryonic to extra-embryonic endoderm stem cells reveals distinct differentiation capacities of pluripotent stem cell states.
    Authors: Cho Et al.
    Cancer Biol Ther 2012;139:2866

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