AMG 548

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Cat.No. 3920 - AMG 548 | C29H27N5O | CAS No. 864249-60-5
Description: Potent and selective p38α inhibitor
Chemical Name: 2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (4)
Pathways (1)

Biological Activity

Potent and selective inhibitor of p38α (Ki values are 0.5, 3.6, 2600 and 4100 nM for p38α, p38β, p38γ and p38δ respectively). Displays >1000-fold selectivity against 36 other kinases; inhibits whole blood LPS-stimulated TNFα (IC50 = 3 nM). Efficacious in acute and chronic models of arthritis.

Compound Libraries

AMG 548 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 461.56
Formula C29H27N5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 864249-60-5
PubChem ID 11167112
InChI Key RQVKVJIRFKVPBF-VWLOTQADSA-N
Smiles O=C1N(C)C(NC[C@@H](N)CC5=CC=CC=C5)=NC(C4=CC=NC=C4)=C1C3=CC2=C(C=C3)C=CC=C2

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.8 100
ethanol 49.8 100

Preparing Stock Solutions

The following data is based on the product molecular weight 461.56. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.17 mL 10.83 mL 21.67 mL
5 mM 0.43 mL 2.17 mL 4.33 mL
10 mM 0.22 mL 1.08 mL 2.17 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

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References

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

Dominguez et al (2005) p38 MAP kinase inhibitors: many are made, but few are chosen. Curr.Opin.Drug Discov.Devel. 8 421 PMID: 16022178

Lee and Dominguez (2005) MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38α protein. Curr.Med.Chem. 12 2979 PMID: 16378500


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Keywords: AMG 548, AMG 548 supplier, AMG548, potent, selective, p38alpha, p38a, p38α, inhibitors, inhibits, p38, 3920, Tocris Bioscience

1 Citation for AMG 548

Citations are publications that use Tocris products. Selected citations for AMG 548 include:

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


Do you know of a great paper that uses AMG 548 from Tocris? Please let us know.

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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* or download your copy today!

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


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
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
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
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 AMG 548

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.