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Documentos

PZ0181

Sigma-Aldrich

PD184352

≥98% (HPLC)

Sinónimos:

2-(2-Chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide, CI-1040

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About This Item

Fórmula empírica (notación de Hill):
C17H14ClF2IN2O2
Número de CAS:
212631-79-3
Peso molecular:
478.66
MDL number:
MFCD02683961
UNSPSC Code:
51111800
PubChem Substance ID:
329823755
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

white to tan

solubility

DMSO: ≥30 mg/mL

storage temp.

room temp

SMILES string

Fc1ccc(C(=O)NOCC2CC2)c(Nc3ccc(I)cc3Cl)c1F

InChI

1S/C17H14ClF2IN2O2/c18-12-7-10(21)3-6-14(12)22-16-11(4-5-13(19)15(16)20)17(24)23-25-8-9-1-2-9/h3-7,9,22H,1-2,8H2,(H,23,24)

InChI key

GFMMXOIFOQCCGU-UHFFFAOYSA-N

Gene Information

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

Biochem/physiol Actions

PD184352 (CI-1040) is a highly selective non-competitive inhibitor of MEK (MKK1; MAPK kinase) and the closely related MKK2. It has anti-cancer activity, suppresses the ERK pathway, and has been used along with other classes of inhibitors to establish embryonic stem cell lines.

Features and Benefits

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

pictograms

Environment
GHS09

signalword

Warning

hcodes

H400

Hazard Classifications

Aquatic Acute 1

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Kazushi Watanabe et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 16(4), 1170-1178 (2010-02-11)
The extracellular signal-regulated kinase (ERK) pathway is upregulated in human cancers and represents a target for mechanism-based approaches to cancer treatment. However, specific blockade of the ERK pathway alone induces mostly cytostatic rather than proapoptotic effects, resulting in a limited
Raymond R Mattingly et al.
The Journal of pharmacology and experimental therapeutics, 316(1), 456-465 (2005-10-22)
Type 1 neurofibromatosis (NF1) is a common autosomal dominant disorder that results in neuroectodermal tumors. The NF1 tumor-suppressor gene encodes neurofibromin, which includes a GTPase-activating domain for Ras inactivation. Affinity purification showed N-Ras to be the predominant activated isoform of
Yanli Li et al.
European journal of pharmacology, 818, 167-173 (2017-10-28)
Clonidine, a classical α-2 adrenergic agonists, has been shown to antagonize brain damage caused by hypoxia, cerebral ischemia and excitotoxicity and reduce cerebral infarction volume in recent studies. We herein investigate the regulatory effect and possible underlying mechanism of clonidine
Marta Olivera Santa-Catalina et al.
Archives of biochemistry and biophysics, 636, 42-49 (2017-11-12)
Growing evidence suggests that Diabetes Mellitus increases the risk of developing Alzheimer's disease. It is well known that hyperglycemia, a key feature of Diabetes Mellitus, may induce plasma osmolarity disturbances. Both hyperglycemia and hyperosmolarity promote the altered post-translational regulation of
Ons Zakraoui et al.
Molecular carcinogenesis, 56(1), 18-35 (2016-01-30)
Lebein, is an heterodimeric disintegrin isolated from Macrovipera lebetina snake venom that was previously characterized as an inhibitor of ADP-induced platelet aggregation. In this study, we investigated the effect of Lebein on the p53-dependent growth of human colon adenocarcinoma cell
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