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AMG-548

  Cat. No.:  DC20664   Featured
Chemical Structure
864249-60-5
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More than 5000 active chemicals with high quality for research!
Field of application
AMG-548 is a potent and selective inhibitor of p38α with Ki of 0.5 nM, dispalys weak inhibition for p38β (Ki=3.6 nM), and >5,000-fold selectivity over p38γ and p38δ; shows >1,000-fold selectivity over other 36 kinases, and is efficacious in acute and chro
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 864249-60-5
Chemical Name: 2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone
Synonyms: AMG548;AMG 548
SMILES: C1=CC=C(C[C@@H](CNC2=NC(C3=CC=NC=C3)=C(C3C=CC4=CC=CC=C4C=3)C(=O)N2C)N)C=C1
Formula: C29H27N5O
M.Wt: 461.569
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Verkaar F, et al. Chem Biol. 2011 Apr 22;18(4):485-94. 2. Lee MR, et al. Curr Med Chem. 2005;12(25):2979-94. 3. Dominguez C, et al. Curr Opin Drug Discov Devel. 2005 Jul;8(4):421-30.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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