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Dokumente

SML3800

Sigma-Aldrich

Selumetinib

≥98% (HPLC)

Synonym(e):

5-((4-Bromo-2-chlorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide, 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, ARRY 142886, ARRY-142886, ARRY142886, AZD 6244, AZD-6244, AZD6244

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About This Item

Empirische Formel (Hill-System):
C17H15BrClFN4O3
CAS-Nummer:
606143-52-6
Molekulargewicht:
457.68
MDL-Nummer:
MFCD11977472
UNSPSC-Code:
12352200
NACRES:
NA.21

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear (Warmed)

Lagertemp.

2-8°C

Biochem./physiol. Wirkung

Selumetinib (ARRY-142886; AZD6244) is an orally active, potent and selective MEK1/2 inhibitor (MEK1 IC50 = 14 nM; <20% inhibition of >40 other kinases at 10 µM) that effectively downregulates cellular ERK1/2 phosphorylation levels (IC50 <40 nM post 1h incubation using 5 different cell lines). Selumetinib inhibits MEK1/2-dependent proliferations in cancer cultures (IC50 in nM = 59/Malme-3M, 93/SK-MEL-28, 175/HT-29, 200/SK-MEL-2, 473/MIA PaCa-2) and exhibits anti-tumor efficacy in mice in vivo (10-100 mg/kg p.o. b.i.d.; BxPC3 & HT-29 xenograft models).

Piktogramme

Health hazardExclamation mark
GHS08,GHS07

Signalwort

Warning

Gefahreneinstufungen

Acute Tox. 4 Oral - Aquatic Chronic 4 - Repr. 2 - Skin Sens. 1 - STOT RE 2

Zielorgane

Gastrointestinal tract,Eyes,Urinary tract

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 2

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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Barry R Davies et al.
Molecular cancer therapeutics, 6(8), 2209-2219 (2007-08-19)
Constitutive activation of the extracellular signal-regulated kinase 1/2 (ERK1/2) mitogen-activated protein kinase (MAPK) signaling pathway in human cancers is often associated with mutational activation of BRAF or RAS. MAPK/ERK kinase 1/2 kinases lie downstream of RAS and BRAF and are
Nikolas K Haass et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 14(1), 230-239 (2008-01-04)
Disseminated melanoma is highly therapy resistant. The finding that 66% of melanomas harbor the activating BRAF(V600E) mutation has raised expectations for targeting the Ras/RAF/mitogen-activated protein (MAP)/extracellular signal-regulated kinase (ERK) kinase (MEK)/ERK pathway in melanoma. This study addresses the anti-melanoma activity
Tammie C Yeh et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 13(5), 1576-1583 (2007-03-03)
The Ras-Raf-mitogen-activated protein kinase kinase (MEK) pathway is overactive in many human cancers and is thus a target for novel therapeutics. We have developed a highly potent and selective inhibitor of MEK1/2. The purpose of these studies has been to

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