FR 180204

Pricing Availability Delivery Time Qty
Cat.No. 3706 - FR 180204 | C18H13N7 | CAS No. 865362-74-9
Description: Selective ERK inhibitor
Chemical Name: 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
Purity: ≥98% (HPLC)
Datasheet
Citations (7)
Literature
Pathways

Biological Activity

Selective ERK inhibitor (IC50 values are 0.14 and 0.31 μM for ERK2 and ERK1 respectively). Displays 30-fold selectivity for ERK over p38α (IC50 = 10 μM); displays no activity against human recombinant MEK1, MKK4, IKKα, PKCα, Src, Syc and PDGFα at concentrations less than 30 μM. Also inhibits TGFβ-induced AP-1 activation in Mv1Lu cells (IC50 = 3.1 μM).

Compound Libraries

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Technical Data

M. Wt 327.34
Formula C18H13N7
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 865362-74-9
PubChem ID 11493598
InChI Key XVECMUKVOMUNLE-UHFFFAOYSA-N
Smiles NC1=NNC2=C1C=C(C3=C(C=CC=C5)N5N=C3C4=CC=CC=C4)N=N2

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 32.73 100

Preparing Stock Solutions

The following data is based on the product molecular weight 327.34. 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 3.05 mL 15.27 mL 30.55 mL
5 mM 0.61 mL 3.05 mL 6.11 mL
10 mM 0.31 mL 1.53 mL 3.05 mL
50 mM 0.06 mL 0.31 mL 0.61 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Ohori et al (2005) Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem.Biophys.Res.Comm. 336 357 PMID: 16139248

Perrett et al (2013) Signaling to Extracellular Signal-regulated Kinase from ErbB1 Kinase and Protein Kinase C. J Biol Chem. 19 288 PMID: 23754287


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Keywords: selective ERK inhibitors inhibits MAPK signalling signaling ERK1 ERK2 FR180204 ERK

7 Citations for FR 180204

Citations are publications that use Tocris products. Selected citations for FR 180204 include:

Shamblott et al (2016) Neurogenin 3 is regulated by neurotrophic tyrosine kinase receptor type 2(TRKB) signaling in the adult human exocrine pancreas. Cell Communication and Signaling 14 23 PMID: 27659207

You et al (2015) Inhibition of ERK1/2 down-regulates the Hippo/YAP signaling pathway in human NSCLC cells. Oncotarget 6 4357 PMID: 25738359

Wurm et al (2015) Terminal epidermal differentiation is regulated by the interaction of Fra-2/AP-1 with Ezh2 and ERK1/2. PLoS Biol 29 144 PMID: 25547114

López-Cotarelo et al (2015) A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells. Proc Natl Acad Sci U S A 290 827 PMID: 25425646

Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Microvasc Res 171 5417 PMID: 25052197

Eckle et al (2013) HIF1A reduces acute lung injury by optimizing carbohydrate metabolism in the alveolar epithelium. J Biol Chem 11 e1001665 PMID: 24086109

Shaw and Lloyd (2012) Post-transcriptional regulation of placenta growth factor mRNA by hydrogen peroxide. Genes Dev 84 155 PMID: 22683469


Do you know of a great paper that uses FR 180204 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

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  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
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Immunology

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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
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Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

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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 FR 180204

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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