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Submit ReviewPD 0325901
Description: Potent inhibitor of MEK1/2
Alternative Names: PD325901
Chemical Name: N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide
Purity: ≥99% (HPLC)
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.
Compound Libraries
PD 0325901 is also offered as part of the Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 482.19 |
| Formula | C16H14F3IN2O4 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 391210-10-9 |
| PubChem ID | 9826528 |
| InChI Key | SUDAHWBOROXANE-SECBINFHSA-N |
| Smiles | FC1=CC(I)=CC=C1NC2=C(C(NOC[C@H](O)CO)=O)C=CC(F)=C2F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 12.05 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 482.19. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 8.3 mL | 41.48 mL | 82.95 mL |
| 1.25 mM | 1.66 mL | 8.3 mL | 16.59 mL |
| 2.5 mM | 0.83 mL | 4.15 mL | 8.3 mL |
| 12.5 mM | 0.17 mL | 0.83 mL | 1.66 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Barrett et al (2008) The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg.Med.Chem.Lett. 18 6501 PMID: 18952427
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
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
Lin et al (2009) A chemical platform for improved induction of human iPSCs. Nat.Methods. 6 805 PMID: 19838168
Koehler et al (2014) 3D mouse embryonic stem cell culture for generating inner ear organoids. Nat.Protoc. 9 1299 PMID: 24784820
If you know of a relevant reference for PD 0325901, please let us know.
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20 Citations for PD 0325901
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
Zhang et al (2019) Implantation initiation of self-assembled embryo-like structures generated using three types of mouse blastocyst-derived stem cells. Nat Commun 10 496 PMID: 30700702
Stumpf et al (2017) Stem Cell Differentiation as a Non-Markov Stochastic Process. Cell Syst 5 268 PMID: 28957659
Yang et al (2017) Establishment of mouse expanded potential stem cells. Nature 550 393 PMID: 29019987
Tuck et al (2018) Distinctive features of lincRNA gene expression suggest widespread RNA-independent functions. Life Sci Alliance 1 e201800124 PMID: 30456373
Liu et al (2018) CRISPR-based chromatin remodeling of the endogenous Oct4 or Sox2 locus enables reprogramming to pluripotency. Cell Stem Cell. 22 252 PMID: 29358044
Caires-Júnior (2018) Discordant congenital Zika syndrome twins show differential in vitro viral susceptibility of neural progenitor cells. Nat Commun 9 475 PMID: 29396410
Wang (2018) Gain of toxic apolipoprotein E4 effects in human iPSC-derived neurons is ameliorated by a small-molecule structure corrector. Nat Med 24 647 PMID: 29632371
Zawily et al (2016) The intrinsically kinase-inactive EPHB6 receptor predisposes cancer cells to DR5-induced apoptosis by promoting mitochondrial fragmentation. Oncotarget 7 77865 PMID: 27788485
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
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
Jullien et al (2017) Gene Resistance to Transcriptional Reprogramming following Nuclear Transfer Is Directly Mediated by Multiple Chromatin-Repressive Pathways. Mol Cell 65 873 PMID: 28257702
Holland et al (2015) Effects of AKT inhibition on HGF-mediated erlo. resistance in non-small cell lung cancer cell lines. J Cancer Res Clin Oncol 141 615 PMID: 25323938
Kearns et al (2015) Functional annotation of native enhancers with a Cas9-histone demethylase fusion. Nat Methods 12 401 PMID: 25775043
Maza et al (2015) Transient acquisition of pluripotency during somatic cell transdifferentiation with iPSC reprogramming factors. Nat Biotechnol 33 769 PMID: 26098448
Gupta et al (2017) PARK2 Depletion Connects Energy and Oxidative Stress to PI3K/Akt Activation via PTEN S-Nitrosylation. Mol Cell 65 999 PMID: 28306514
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
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
Sladitschek and Neveu (2015) The bimodally expressed microRNA miR-142 gates exit from pluripotency. J Neuroinflammation 11 850 PMID: 26690966
Do you know of a great paper that uses PD 0325901 from Tocris? Please let us know.
Reviews for PD 0325901
Average Rating: 5 (Based on 3 Reviews.)
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2i conditions for mES cells.
By
Anonymous on 08/20/2019
Assay Type: In Vivo
Species: Mouse
Used to grow mES cells in 2i conidtions. The cells grew well and I did QPCR on isolated RNA
Mmaintenance of naive pluripotency in 2i.
By
Megha PB on 07/18/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: E14TG2a
Mouse ES cells in 2i remain to be in the naive pluripotent state while cells in -2i for 48 hours exit naive pluripotency
Great inhibitor for ERK signaling.
By
Anonymous on 12/08/2017
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Primary mouse lung endothelial cells
Primary lung endothelial cells were pretreated with various concentrations of PD 0325901 for 30 minutes prior to the treatment of IL1b (1ng/ml).
24 hours later, cell was lyzed and analyzed by western blot. Lane 1: PBS controlLane 2: + PD 0326901 100nMLane 3: + PD 0326901 10nM
Protocols for PD 0325901
The following protocols feature additional information for the use of PD 0325901 (Cat. No. 4192).
Literature in this Area
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MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for PD 0325901
