PD 198306

Pricing Availability Delivery Time Qty
Cat.No. 2605 - PD 198306 | C18H16F3IN2O2 | CAS No. 212631-61-3
Description: Selective inhibitor of MEK1/2
Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature
Pathways

Biological Activity

Potent inhibitor of MEK1/2. Inhibits isolated enzyme at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at concentrations of 30 - 100 nM. Highly selective for MEK; IC50 values are > 1, > 4, > 4 and > 10 μM for ERK, c-Src, cdks and PI 3-kinase γ respectively. Antihyperalgesic; blocks static allodynia in the streptozocin model of neuropathic pain following i.t. administration.

Technical Data

M. Wt 476.23
Formula C18H16F3IN2O2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 212631-61-3
PubChem ID 9956637
InChI Key UHAXDAKQGVISBZ-UHFFFAOYSA-N
Smiles CC1=C(NC2=C(C=C(F)C(F)=C2F)C(=O)NOCC2CC2)C=CC(I)=C1

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 47.62 100
ethanol 47.62 100

Preparing Stock Solutions

The following data is based on the product molecular weight 476.23. 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 2.1 mL 10.5 mL 21 mL
5 mM 0.42 mL 2.1 mL 4.2 mL
10 mM 0.21 mL 1.05 mL 2.1 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.

Ciruela et al (2003) Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br.J.Pharmacol. 138 751 PMID: 12642375

Pelletier et al (2003) In vivo selective inhibition of mitogen-activated protein kinase kinase 1/2 in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes. Arthrit.Rheumat. 48 1582 PMID:


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Keywords: PD 198306, supplier, Selective, inhibitors, inhibits, MEK1/2, Mitogen-Activated, Protein, Kinase, kinases, PD198306, MEK, Tocris Bioscience

1 Citation for PD 198306

Citations are publications that use Tocris products. Selected citations for PD 198306 include:

Ripple et al (2013) Acute mitochondrial inhibition by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) 1/2 inhibitors regulates proliferation. J Biol Chem 288 2933 PMID: 23235157


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Reviews

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Literature in this Area

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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
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Kinases

Kinases Product Listing

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

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  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
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Pain

Pain Research Product Guide

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

  • Nociception
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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 198306

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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