AMG 548

Modify Date: 2024-01-31 13:16:56

AMG 548 Structure
AMG 548 structure
Common Name AMG 548
CAS Number 864249-60-5 Molecular Weight 461.55800
Density N/A Boiling Point N/A
Molecular Formula C29H27N5O Melting Point N/A
MSDS Chinese USA Flash Point N/A

 Use of AMG 548


AMG-548 is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) [1]. AMG-548 inhibits Wnt signaling by direcly inhibing Casein kinase 1 isoforms δ and ε[2].

 Names

Name 2-(((2S)-2-amino-3-phenylpropyl)amino)-3-methyl-5-(2-naphthyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone
Synonym More Synonyms

 AMG 548 Biological Activity

Description AMG-548 is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) [1]. AMG-548 inhibits Wnt signaling by direcly inhibing Casein kinase 1 isoforms δ and ε[2].
Related Catalog
Target

p38α:0.5 nM (Ki)

p38β:3.6 nM (Ki)

CK1

In Vivo AMG-548 has rat F of 62% and dog F of 47%. The t1/2 is 4.6 hours in rats and 7.3 hours in dogs[1].
References

[1]. Lee MR, et al. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alphaprotein. Curr Med Chem. 2005;12(25):2979-94.

[2]. Verkaar F, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94.

 Chemical & Physical Properties

Molecular Formula C29H27N5O
Molecular Weight 461.55800
Exact Mass 461.22200
PSA 85.83000
LogP 5.41770

 Safety Information

Hazard Codes Xi

 Synonyms

AMG 548
(S)-2-(2-amino-3-phenylpropylamino)-1-methyl-5-(2-naphthyl)-4-(4-pyridyl)pyrimidine-6-one
2-[[(2S)-2-amino-3-phenylpropyl]amino]-3-methyl-5-naphthalen-2-yl-6-pyridin-4-ylpyrimidin-4-one
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: AMG-548
  • Price: $850.0/100mg $1700.0/250mg $3600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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