PD 0325901

Cat. No. 4192

PD 0325901 C16H14F3IN2O4 [391210-10-9]

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Alternative Name: 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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Ciuffreda et al (2009) Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations. Neoplasia 11 720. PMID: 19649202.

Lin et al (2009) A chemical platform for improved induction of human iPSCs. Nat.Methods. 6 805. PMID: 19838168.

Barrett et al (2008) The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg.Med.Chem.Lett. 18 6501. PMID: 18952427.

Sebolt-Leopold et al (2004) The biological profile of PD 0325901: a second generation analog of CI-1040 with improved pharmaceutical potential. Proc.Amer.Assoc.Cancer Res. 45 925.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for PD 0325901 include:

Oliveira et al (2016) Poly(I:C) increases the expression of mPGES-1 and COX-2 in rat primary microglia. Stem Cells 13 11. PMID: 26780827.

Kearns et al (2015) Functional annotation of native enhancers with a Cas9-histone demethylase fusion. Nat Methods 12 401. PMID: 25775043.

Mattis et al (2015) HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity. PLoS One 24 3257. PMID: 25740845.

Maza et al (2015) Transient acquisition of pluripotency during somatic cell transdifferentiation with iPSC reprogramming factors. Nat Biotechnol 33 769. PMID: 26098448.

Sladitschek and Neveu (2015) The bimodally expressed microRNA miR-142 gates exit from pluripotency. J Neuroinflammation 11 850. PMID: 26690966.

Solari et al (2015) Manganese Superoxide Dismutase Gene Expression Is Induced by Nanog and Oct4, Essential Pluripotent Stem Cells' Transcription Factors. Mol Syst Biol 10 e0144336. PMID: 26642061.

Muthusamy et al (2014) A method to identify and isolate pluripotent human stem cells and mouse epiblast stem cells using lipid body-associated retinyl ester fluorescence. Stem Cell Reports 3 169. PMID: 25068130.

Cho et al (2012) Conversion from mouse embryonic to extra-embryonic endoderm stem cells reveals distinct differentiation capacities of pluripotent stem cell states. Cancer Biol Ther 139 2866. PMID: 22791892.

Denham et al (2012) 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. Development 30 2400. PMID: 22911885.

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Keywords: PD 0325901, supplier, pfizer, PD0325901, PD325901, mek1, mek2, mkk1, mkk2, mapk, signalling, signaling, selective, inhibitors, inhibits, proapoptotic, organoids, Tocris Bioscience, MEK Inhibitor products

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