882663-88-9 AMG-47a AKSci SYN1007
 
 
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  SYN1007    
AMG-47a
, >95%
 
AMG47a




IDENTITY
CAS Number:882663-88-9
MDL Number:MFCD09970318
MF:C29H28F3N5O2
MW:535.56
SPECIFICATIONS & PROPERTIES
Purity:>95%
Long-Term Storage:Store at room temperature

BIOLOGICAL INFO
Solubility:15 mM in DMSO
Application(s):LIMK

REVIEW

 The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling mediated by the T cell receptor (TCR), which leads to normal T cell development and activation. Selective inhibition of Lck is expected to offer a new therapy for the treatment of T-cell-mediated autoimmune and inflammatory disease. AMG-47 is one of two optimized chemical compounds that has been shown to be extremely effective in vivo and in vitro in inhibiting Lck as well as a number of other receptor tyrosine kinases. In an anti-CD3/ IL-2 mouse model system AMG-47 has been shown to be effective in inhibiting the Lck mediated anti-inflammatory activity (ED50 11 mg/kg; 630nM) in vivo. In multiple other in vitro assays, AMG-47 exhibits subnanomolar inhibition against Lck, and low (<10nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK alpha (p38alpha). Moreover at slightly higher doses but well under 10µM, AMG-47 effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2μM.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of June 26, 2019


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