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PZ0162 Sigma-Aldrich

PD 0325901

≥98% (HPLC)

Synonym: N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide

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Properties

Related Categories Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Fluorination Ready Pharma-Developed Compounds,
Quality Level   100
assay   ≥98% (HPLC)
form   powder
optical activity   [α]/D -1.8 to -3.5°, c = 1 mg/mL in methanol
mfr. no.   Pfizer®
color   white to off-white
solubility   DMSO: 20 mg/mL, clear
originator   Pfizer
storage temp.   2-8°C
SMILES string   OC[C@@H](O)CONC(=O)c1ccc(F)c(F)c1Nc2ccc(I)cc2F
InChI   1S/C16H14F3IN2O4/c17-11-3-2-10(16(25)22-26-7-9(24)6-23)15(14(11)19)21-13-4-1-8(20)5-12(13)18/h1-5,9,21,23-24H,6-7H2,(H,22,25)/t9-/m1/s1
InChI key   SUDAHWBOROXANE-SECBINFHSA-N
Gene Information   human ... MAP2K1(5604), MAP2K2(5605)

Description

Application

PD 0325901 has been used as an inhibitor in extracellular signal-regulated kinase (ERK) inhibition assay in primed induced pluripotent stem cells, RKO colorectal cancer cell line and human embryonic stem cells(hESCs).

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

PD 0325901 by inhibiting mitogen-activated protein kinases (MAPKs) elicits growth-inhibitory and antiangiogenic effects on glioblastoma and melanoma tumor progression.

PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. The Ki is 1.1 and 0.79 nM for MEK1 and MEK2, respectively. PD 0325901 was inactive against a panel of 27 other kinases. PD 0325901 inhibited C26 tumor pERK by 75% when dosed at 25 mg/kg in mice.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®Pfizer), a collection of 90 Pfizer-developed drugs and research tools. Click here to learn more.

This compound is featured on the MAPKKKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Other Notes

This compound was developed by Pfizer for Kinase Phosphatase Biology research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Pfizer is a registered trademark of Pfizer, Inc.

Safety & Documentation

Safety Information

Symbol 
Signal word 
Danger
Hazard statements 
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

MAPKKKs

Mitogen-activated protein kinase (MAPK) signaling pathways mediate cellular responses to many stimuli including growth factors, hormones, cytokines and environmental stresses. MAPK pathways can be di...
Keywords: Apoptosis, Cancer, Degradations, Environmental, Growth factors, Hormones, Inflammation, Phosphorylations, RNA immunoprecipitation, Ubiquitinations

Naive Pluripotent Stem Cell Culture in an Inhibitor Based 2i/LIF Containing Serum-Free and Feeder-Free Stem Cell Media

Naive pluripotent stem cells are located within the epiblast of mature blastocysts. These primitive “ground-state” cells may be cultured in vitro using specialized media and small molecule inhibitors...
Gabi Tremml, Ming Li and Vi Chu1*,
1MilliporeSigma, Bioscience Division, Temecula, CA, USA
 
Keywords: Cell culture, Gene expression, Immunocytochemistry, Microscopy, Polymerase chain reaction, Polymerase chain reaction - quantitative, Transcription

Pfizer Compounds for Kinase Phosphatase Biology

From our library of Articles, Sigma-Aldrich presents Pfizer Compounds for Kinase Phosphatase Biology

The Role of Inflammation in Neurodegeneration

It is well established that the brain can sense and react to peripheral insults through the rapid induction of fever and other neuroendocrine changes in response to events such as infection and tissu...
Scott Hauser, Technology Transfer Specialist, Sigma® Life Science
Biofiles, Vol. 8, No. 19
Keywords: Adhesion, Central Nervous System, Diseases, Gene expression, Inflammation, Neurodegenerative Diseases, Reductions

Peer-Reviewed Papers
15

References

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