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Merck

PZ0162

Sigma-Aldrich

PD 0325901

≥98% (HPLC)

Sinónimos:

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

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About This Item

Fórmula empírica (notación de Hill):
C16H14F3IN2O4
Número de CAS:
Peso molecular:
482.19
Número MDL:
Código UNSPSC:
12352200
ID de la sustancia en PubChem:

Análisis

≥98% (HPLC)

formulario

powder

actividad óptica

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

color

white to off-white

solubilidad

DMSO: 20 mg/mL, clear

temp. de almacenamiento

2-8°C

cadena SMILES

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

Clave InChI

SUDAHWBOROXANE-SECBINFHSA-N

Información sobre el gen

Aplicación

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).

Acciones bioquímicas o fisiológicas

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.

Características y beneficios

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

Pictogramas

Skull and crossbonesHealth hazard

Palabra de señalización

Danger

Frases de peligro

Clasificaciones de peligro

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

Código de clase de almacenamiento

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

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Visite la Librería de documentos

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)

Artículos

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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