FR 180204

Pricing Availability   Qty
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 (11)
Reviews (2)
Literature (4)
Pathways (1)

Biological Activity for FR 180204

FR 180204 is a 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 for FR 180204

FR 180204 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for FR 180204

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for FR 180204

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 32.73 100

Preparing Stock Solutions for FR 180204

The following data is based on the product molecular weight 327.34. Batch specific molecular weights may vary from batch to batch due to the degree 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 for FR 180204

Certificate of Analysis / Product Datasheet
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References for FR 180204

References are publications that support the biological activity of the product.

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


If you know of a relevant reference for FR 180204, please let us know.

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Keywords: FR 180204, FR 180204 supplier, selective, ERK, inhibitors, inhibits, MAPK, signalling, signaling, ERK1, ERK2, FR180204, 3706, Tocris Bioscience

11 Citations for FR 180204

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

Yuede et al (2021) Pimavanserin, a 5HT 2A receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer's disease. J.Neurochem. 156 658 PMID: 33278025

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

Chaikuad et al (2014) A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nat Chem Biol 10 853 PMID: 25195011

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? Please let us know.

Reviews for FR 180204

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Used to block ERK signaling..
By MARINA KOUTSIOUMPA on 10/13/2022
Assay Type: In Vitro
Species: Human

Pancreatic cancer cells were pretreated for 2 hours with FR 180204 followed by conventional chemotherapeutics. MEK inhibition had an additive effect on cancer cell’s viability upon 3 days of treatment.


FR 180204 blocks LPA induced COX-2 expression.
By Anonymous on 12/13/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma

MG-63 cells were pre-incubated with 10 µM FR 180204 for 30 min followed by treatment with 10 µM LPA for 3 h to follow COX-2 expression using Western blot. FR 180204 inhibited COX-2 induction by LPA.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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MAPK Signaling Scientific Review

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Pathways for FR 180204

MAPK Signaling Pathway

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.