FR 180204

Catalog No.S7524

FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively.

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FR 180204 Chemical Structure

FR 180204 Chemical Structure
Molecular Weight: 327.34

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Product Description

Biological Activity

Description FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively.
Targets ERK2 [1] ERK1 [1]
IC50 0.14 μM(Ki) 0.31 μM(Ki)
In vitro In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC50 of 3.1 μM. [1] FR 180204 inhibits spontaneous mesothelioma cell growth. [3]
In vivo In collagen-induced arthritis mice, FR180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss. [2] In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves Clinical parameters. [4]
Features ERK1/ERK2-selective inhibitor

Protocol(Only for Reference)

Kinase Assay: [1]

ERK assay Nunc-Immuno MaxiSorp plates are coated with 20 μg/ml MBP solution in phosphate-buffered saline (PBS). After washing with PBS containing 0.05% Tween 20 (T-PBS), blocking buffer (T-PBS containing 3% BSA) is added to each well and the plates are incubated for 10 min at room temperature. After washing with T-PBS, chemical compounds, ATP and recombinant ERK2 diluted in assay dilution buffer (20 mM Mops, pH 7.2, 25 mM β-glycerol phosphate, 5 mM EGTA, 1 mM sodium orthovanadate, 1 mM dithiothreitol, and 50 μg/ml BSA) and are added to each well. Vehicle groups (containing 0.1% DMSO) and kinase-withdrawal groups are used for the control and basal determinations. After incubation for 1 h at room temperature, plates are washed twice with T-PBS. Anti-phospho MBP antibody (0.2 μg/ml) is added to each well, and the plates are incubated for 1 h at room temperature. After washing, anti-mouse HRP-conjugated polyclonal antibodies are added and the plates were incubated for 30 min. SuperSignal chemiluminescent substrate is used for the measurement of HRP activity according to the manufacturer’s instructions. Prism 4.0 software is used for the Lineweaver–Burk plot analysis, IC50 and Ki determinations.

Cell Assay: [3]

Cell lines Met5A, MSTO-211H, NCI-H28, NCI-H2052, and NCIH2452 cell lines
Concentrations 10 μM
Incubation Time 48 hours
Method Cell viability is assayed by the method using MTT. MTT-reactive cells are quantified at an absorbance of 570 nm using a micro-plate reader.

Animal Study: [2]

Animal Models Collagen-induced arthritis mouse model
Formulation Suspended in 0.1% methylcellulose solution
Dosages 100 mg/kg
Administration i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Ohori M, et al. Biochem Biophys Res Commun. 2005, 336(1), 357-363.

[2] Ohori M, et al. Naunyn Schmiedebergs Arch Pharmacol. 2007, 374(4), 311-316.

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Chemical Information

Download FR 180204 SDF
Molecular Weight (MW) 327.34
Formula

C18 H13 N7

CAS No. 865362-74-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 65 mg/mL (198.57 mM)
Ethanol 2 mg/mL warming (6.1 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1H-​Pyrazolo[3,​4-​c]​pyridazin-​3-​amine, 5-​(2-​phenylpyrazolo[1,​5-​a]​pyridin-​3-​yl)​-

Customer Product Validation(1)


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Rating
Source Biochem Biophys Res Commun, 2015, 459(3): 398-404. FR 180204 purchased from Selleck
Method Western Blot
Cell Lines H1299-EML4-ALK cells
Concentrations 10 μM
Incubation Time 24 h
Results Consistent with this observation, We showed that the selected inhibitor FR180204, effectively inhibiting ERK1/2 phosphorylation at a concentration of 10 μmol/L, resulted increased expression of E-cadherin.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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