864249-60-5

864249-60-5 structure

Name: AMG 548
Chemical Name: 2-(((2S)-2-amino-3-phenylpropyl)amino)-3-methyl-5-(2-naphthyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone
CAS Number: 864249-60-5
Molecular Formula: C₂₉H₂₇N₅O
Molecular Weight: 461.55800
Catalog: Signaling Pathways Cell Cycle/DNA Damage Casein Kinase
Create Date: 2018-04-02 00:21:15
Modify Date: 2024-01-31 13:16:56
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].

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

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	Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK Research Areas >> Inflammation/Immunology Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase
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.

Hazard Codes	Xi