FR 180204

Tocris Bioscience | Catalog # 3706

Selective ERK inhibitor
Tocris Bioscience
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Key Product Details

Description

Selective ERK inhibitor

Product Description

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).

Product Specifications for FR 180204

Molecular Weight

327.34

Formula

C18H13N7

Storage

Store at +4°C

Purity

≥98% (HPLC)

Chemical Name

5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine

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.

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Solubility

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 all 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

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 94 publications citing the usage of this product.

Product Documents for FR 180204

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for FR 180204

For research use only

Customer Reviews for FR 180204 (2)

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  • Used to block ERK signaling.
    Name: MARINA KOUTSIOUMPA
    Species: Human
    Assay Type: In Vitro
    Verified Customer | Posted 10/13/2022
    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
    Name: Anonymous
    Species: Human
    Assay Type: In Vitro
    Cell Line/Tissue: Osteosarcoma
    Verified Customer | Posted 12/13/2018
    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.
    FR 180204 3706

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