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Merck
CN

PZ0162

PD 0325901

≥98% (HPLC), MKK1 (MEK1) and MKK2 (MEK2) inhibitor, powder

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C16H14F3IN2O4
CAS Number:
391210-10-9
Molecular Weight:
482.19
PubChem Substance ID:
329823743
UNSPSC Code:
12352200
MDL number:
MFCD08435926
NACRES:
NA.28

Key Documents

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Product Name

PD 0325901, ≥98% (HPLC)

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

SMILES string

FC1=C(NC2=CC=C(I)C=C2F)C(C(NOC[C@H](O)CO)=O)=CC=C1F

InChI key

SUDAHWBOROXANE-SECBINFHSA-N

assay

≥98% (HPLC)

form

powder

optical activity

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

color

white to off-white

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Gene Information

human ... MAP2K1(5604), MAP2K2(5605)

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).

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

Other Notes

2024 CiteAb Award Winner for Supplier Succeeding in Parkinson′s Research

pictograms

Skull and crossbonesHealth hazard
GHS06,GHS08

signalword

Danger

Hazard Classifications

Acute Tox. 3 Oral - Aquatic Chronic 4 - STOT RE 2

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000338680
0000243126
0000338680
0000243126
0000212164

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Resveratrol promotes human embryonic stem cells self-renewal by targeting SIRT1-ERK signaling pathway
Safaeinejad Z, et al.
European Journal of Cell Biology, 96(7), 665-672 (2017)
The role of autophagy in the treatment of BRAF mutant colorectal carcinomas differs based on microsatellite instability status
Koustas E, et al.
PLoS ONE, 13(11), e0207227-e0207227 (2018)
Kimita Suyama et al.
Cancer research, 78(1), 103-114 (2017-10-19)
The Akt pathway is a well-known promoter of tumor malignancy. Akt3 is expressed as two alternatively spliced variants, one of which lacks the key regulatory serine 472 phosphorylation site. Whereas the function of full-length Akt3 isoform (Akt3/+S472) is well-characterized, that
Feeder-Free Derivation of Naive Human Pluripotent Stem Cells
Ward E, et al.
Stem Cells and Development, 26(15), 1087-1089 (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
View All Related Papers

Articles

MAPKKKs

The extracellular signal regulated kinase (ERK1 and ERK2) pathways are activated by mitogens and play an important role in controlling cell growth and differentiation.

Naive Pluripotent Stem Cell Culture in Serum-Free Media

Naive pluripotent stem cells cultured in vitro using specialized media and inhibitors mimic "ground-state" cells from blastocysts.

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