PD 184352

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Cat.No. 4237 - PD 184352 | C17H14ClF2IN2O2 | CAS No. 212631-79-3
Description: Selective MEK inhibitor
Alternative Names: CI-1040
Chemical Name: 2-[(2-Chloro-4-iodophenyl)amino]-N-cyclopropylmethoxy)-3,4-difluorobenzamide
Datasheet
Citations (3)
Literature
Pathways

Biological Activity

Selective MEK inhibitor (Ki = 300 nM in vitro). Suppresses FGF-mediated angiogenesis in vivo and decreases VEGF expression. Enhances the therapeutic efficacy of taxol (Cat. No. 1097) in vivo. Orally active.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 478.66
Formula C17H14ClF2IN2O2
Storage Store at +4°C
CAS Number 212631-79-3
PubChem ID 6918454
InChI Key GFMMXOIFOQCCGU-UHFFFAOYSA-N
Smiles FC1=C(NC2=CC=C(I)C=C2Cl)C(C(NOCC3CC3)=O)=CC=C1F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.87 100
ethanol 11.97 25

Preparing Stock Solutions

The following data is based on the product molecular weight 478.66. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.09 mL 10.45 mL 20.89 mL
5 mM 0.42 mL 2.09 mL 4.18 mL
10 mM 0.21 mL 1.04 mL 2.09 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Allen et al (2003) CI-1040 (PD184252), a targeted signal transduction inhibitor of MEK (MAPKK). Semin.Oncol. 30 105 PMID: 14613031

McDaid et al (2005) Enhancement of the therapeutic efficacy of taxol by the mitogen-activated protein kinase kinase inhibitor CI-1040 in nude mice bearing human heterotransplants. Cancer Res. 65 2854 PMID: 15805287

Solit et al (2006) BRAF mutation predicts sensitivity to MEK inhibition. Nature 439 358 PMID: 16273091


If you know of a relevant reference for PD 184352, please let us know.

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Keywords: pfizer mek1 mek2 mkk1 mkk2 inhibitors inhibits selective mapk signaling signalling map kinases PD184352 CI1040 CI-1040 MEK

3 Citations for PD 184352

Citations are publications that use Tocris products. Selected citations for PD 184352 include:

Wang et al (2015) Activation of protein synthesis in mouse uterine epithelial cells by estradiol-17β is mediated by a PKC-ERK1/2-mTOR signaling pathway. BMC Res Notes 112 E1382 PMID: 25733860

Wouters et al (2014) Central role for protein kinase C in oxytocin and epidermal growth factor stimulated cyclooxygenase 2 expression in human myometrial cells. Genes Cancer 7 357 PMID: 24916153

Martin et al (2014) miR-155 induced transcriptome changes in the MCF-7 breast cancer cell line leads to enhanced mitogen activated protein kinase signaling. J Exp Bot 5 353 PMID: 25352952


Do you know of a great paper that uses PD 184352 from Tocris? If so please let us know.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
MAPK Signaling

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for PD 184352

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

Protocols

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