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Tocris/PD 0325901/4192/10/10 mg

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货号: 4192/10

品牌: Tocris

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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 Technical Data Solubility Calculators Datasheets References

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
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.

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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

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

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