Free shipping on all orders over $ 500

FR 180204

Cat. No. M3642

FR 180204 Structure
Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 155 In stock
50mg USD 720 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

FR180204 inhibited the kinase activity of ERK1 and ERK2, with K(i) values 0.31 and 0.14microM, respectively. FR180204 inhibited TGFbeta-induced luciferase-expression. FR180204 inhibited in vitro CII-induced proliferation of lymph node cells prepared from CII-immunized mice, in which CII-specific T cells are known to undergo specific proliferation.

Protocol
Cell Experiment
Cell lines Met5A, MSTO-211H, NCI-H28, NCI-H2052, and NCIH2452 cell lines
Preparation method Using MTT to assay cell viability . Using a micro-plate reader to quantify MTT-reactive cells at an absorbance of 570 nm.
Concentrations 10 μM
Incubation time 48 hours
Animal Experiment
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)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 327.34
Formula C18H13N7
CAS Number 865362-74-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex.
Ohori M, et al. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63. PMID: 16139248.

Related ERK Products
XMD8-92

XMD8-92 is a potent and selective BMK1/ERK5 inhibitor with Kd of 80 nM.

VRT752271

VRT752271 (BVD-523, Ulixertinib) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

DEL-22379

DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.

XMD17-109

XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 μM in HEK293 cells.

GDC-0994

GDC-0994 is a potent, orally available ERK inhibitor with IC50 1.1 nM and 0.3 nM, respectively.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: FR 180204 supplier, ERK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.