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PZ0181

Sigma-Aldrich

PD184352

≥98% (HPLC)

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Synonym(s):
2-(2-Chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide, CI-1040
Empirical Formula (Hill Notation):
C17H14ClF2IN2O2
CAS Number:
212631-79-3
Molecular Weight:
478.66
MDL number:
MFCD02683961
PubChem Substance ID:
329823755
NACRES:
NA.77

Quality Level

100

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

Signal Word

Warning

Hazard Statements

H400

Precautionary Statements

P273 - P391 - P501

Hazard Classifications

Aquatic Acute 1

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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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
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Genesis (New York, N.Y. : 2000), 48(5), 317-327 (2010-02-18)
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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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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
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