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Safety Information

PZ0162

Sigma-Aldrich

PD 0325901

≥98% (HPLC)

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:
Molecular Weight:
482.19
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:

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

SMILES string

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

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

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. 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.

Pictograms

Skull and crossbonesHealth hazard

Signal Word

Danger

Hazard Statements

Hazard Classifications

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

Storage Class Code

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


Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

ISHL Indicated Name

Substances Subject to be Indicated Names

ISHL Notified Names

Substances Subject to be Notified Names

JAN Code

PZ0162-5MG:4548174001837
PZ0162-25MG:4548174001820
PZ0162-BULK:
PZ0162-VAR:


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Ana Cuadrado et al.
Cell reports, 27(12), 3500-3510 (2019-06-20)
Cohesin exists in two variants carrying either STAG/SA1 or SA2. Here we have addressed their specific contributions to the unique spatial organization of the mouse embryonic stem cell genome, which ensures super-enhancer-dependent transcription of pluripotency factors and repression of lineage-specification genes
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
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)

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.

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.

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