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444966

Sigma-Aldrich

MEK1/2 Inhibitor III

The MEK1/2 Inhibitor III, also referenced under CAS 391210-10-9, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sinónimos:

MEK1/2 Inhibitor III, PD325901, PD0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, MEK Inhibitor III

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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
NACRES:
NA.77

Nivel de calidad

Análisis

≥95% (HPLC)

formulario

solid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
protect from light

color

white to off-white

solubilidad

DMSO: 20 mg/mL

Condiciones de envío

ambient

temp. de almacenamiento

2-8°C

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

Descripción general

A cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo.
A cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo. Also available in InSolution format (Cat. No. 444968).

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Barrett, S.D., et al. 2008. Bioorg. Med. Chem. Lett.18, 6501.
Leyton, J., et al. 2008. Mol. Cancer Ther.7, 3112.
Silva, J., et al. 2008. PLoS Biol.6, 2237.
Ying, Q.L., et al. 2008. Nature453, 519.
Bain, J., et al. 2007. Biochem. J.408, 297.
Solit, D.B., et al. 2006. Nature439, 358.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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


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