PZ0162

Sigma-Aldrich

PD 0325901

≥98% (HPLC)

Synonym(s):
N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide
Empirical Formula (Hill Notation):
C16H14F3IN2O4
CAS Number:
Molecular Weight:
482.19
MDL number:
PubChem Substance ID:

Quality Level

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D -1.8 to -3.5°, c = 1 mg/mL in methanol

manufacturer/tradename

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)

Related Categories

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

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.

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.

Pictograms

Skull and crossbonesHealth hazard

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

Certificate of Analysis
Certificate of Origin
Feeder-Free Derivation of Naive Human Pluripotent Stem Cells
Ward E, et al.
Stem Cells and Development, 26(15), 1087-1089 (2017)
Inhibition of glioblastoma dispersal by the MEK inhibitor PD0325901
Shannon S, et al.
BMC Cancer, 17(1), 121-121 (2017)
Madeleine Linneberg-Agerholm et al.
Development (Cambridge, England), 146(24) (2019-11-20)
Embryonic stem cells (ESCs) exist in at least two states that transcriptionally resemble different stages of embryonic development. Naïve ESCs resemble peri-implantation stages and primed ESCs the pre-gastrulation epiblast. In mouse, primed ESCs give rise to definitive endoderm in response...
Growth-inhibitory and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations
Ciuffreda L, et al.
Neoplasia, 11(8), 720-W6-720-W6 (2009)
Bin Zhang et al.
The Journal of clinical investigation, 126(3), 975-991 (2016-02-16)
Chronic myelogenous leukemia (CML) results from transformation of a long-term hematopoietic stem cell (LTHSC) by expression of the BCR-ABL fusion gene. However, BCR-ABL-expressing LTHSCs are heterogeneous in their capacity as leukemic stem cells (LSCs). Although discrepancies in proliferative, self-renewal, and...
Articles
The extracellular signal regulated kinase (ERK1 and ERK2) pathways are activated by mitogens and play an important role in controlling cell growth and differentiation.
Read More
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.
Read More

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