PD 0325901

Name: PD 0325901
Brand: Tocris Bioscience
SKU: 4192
Rating: 5 (8 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4192

(8)

Citations (323)

COA / SDS

Potent inhibitor of MEK1/2

Key Product Details

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)
Molecular Weight:	482.19

View Full Technical Details for PD 0325901

Technical Data
Citations / Reviews (8)

Biological Activity for PD 0325901

PD 0325901 is a potent MEK1 and MEK2 inhibitor. PD 0325901 inhibits MEK activity in mouse colon 26 cells (IC₅₀ = 0.33 nM). PD 0325901 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. PD 0325901 also inhibits production of proangiogenic cytokines such as VEGF. PD 0325901 enhances generation of induced pluripotent stem cells (iPSCs). PD 0325901 in combination with Vitamin C sustains mouse ES cells at an undifferentiated and hypomethylated state. PD 0325901 promotes myelin recovery in drug-induced demyelination in vivo in mice model. Orally bioavailable. Used in protocols for the generation of CiPSCs from MEFs, induction of cortical neurons from hiPSCs, and culture of mESCs (see below).

For more information about how PD 0325901 may be used, see our protocols: Culturing Transcriptomically Distinct Pluripotent mESCs, Highly Efficient Generation of CiPSCs from MEFs, Accelerated Induction of Cortical Neurons from hiPSCs.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data for PD 0325901

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 for PD 0325901

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	12.05	25

Preparing Stock Solutions for PD 0325901

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	8.30 mL	41.48 mL	82.95 mL
1.25 mM	1.66 mL	8.30 mL	16.59 mL
2.5 mM	0.83 mL	4.15 mL	8.30 mL
12.5 mM	0.17 mL	0.83 mL	1.66 mL

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References for PD 0325901

References are publications that support the biological activity of the product.

Li An alternative culture method to maintain genomic hypomethylation of mouse embryonic stem cells using MEK inhibitor PD0325901 and vitamin C. J.Vis.Exp. 2018 PMID: 29912180
Suo Inhibition of MAPK/ERK pathway promotes oligodendrocytes generation and recovery of demyelinating diseases. Glia 2019 PMID: 30815939
Koehler 3D mouse embryonic stem cell culture for generating inner ear organoids. Nat.Protoc. 2014 PMID: 24784820
Lin A chemical platform for improved induction of human iPSCs. Nat.Methods. 2009 PMID: 19838168
Sebolt-Leopold The biological profile of PD 0325901: a second generation analog of CI-1040 with improved pharmaceutical potential. Proc.Amer.Assoc.Cancer Res.
Ciuffreda Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations. Neoplasia 2009 PMID: 19649202
Barrett The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg.Med.Chem.Lett. 2008 PMID: 18952427