PD 0325901

Pricing Availability Delivery Time Qty
Cat.No. 4192 - PD 0325901 | C16H14F3IN2O4 | CAS No. 391210-10-9
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)
Datasheet
Citations (9)
Literature
Pathways

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.

All Tocris products are intended for laboratory research use only.

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.07 mL 10.37 mL 20.74 mL
5 mM 0.41 mL 2.07 mL 4.15 mL
10 mM 0.21 mL 1.04 mL 2.07 mL
50 mM 0.04 mL 0.21 mL 0.41 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:

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


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9 Citations for PD 0325901

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

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

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

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

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

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

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


Do you know of a great paper that uses PD 0325901 from Tocris? If so please let us know.

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MAPK Signaling Scientific Review

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

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

Protocols

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