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Merck
CN

PZ0181

PD184352

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C17H14ClF2IN2O2
CAS Number:
212631-79-3
Molecular Weight:
478.66
MDL number:
MFCD02683961
UNSPSC Code:
51111800
PubChem Substance ID:
329823755
NACRES:
NA.77

Key Documents

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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 MEK (MKK1; MAPK kinase) inhibitor.
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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Certificates of Analysis (COA)

Lot/Batch Number
0000489028
0000489026
0000489026
0000489028
0000382831

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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
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
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
Shiri Procaccia et al.
Scientific reports, 7, 43078-43078 (2017-02-23)
Crosstalk between the ERK cascade and other signaling pathways is one of the means by which it acquires its signaling specificity. Here we identified a direct interaction of both MEK1 and MEK2 with AKT. The interaction is mediated by the
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