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Chemical Structure| 882663-88-9 Chemical Structure| 882663-88-9

Structure of AMG-47a
CAS No.: 882663-88-9

Chemical Structure| 882663-88-9

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AMG-47a is a Lck inhibitor that can decrease T cell proliferation with anti-inflammatory activity.

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Product Details of AMG-47a

CAS No. :882663-88-9
Formula : C29H28F3N5O2
M.W : 535.56
SMILES Code : O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=C(C)C(C3=CC4=CN=C(NCCN5CCOCC5)N=C4C=C3)=C2
MDL No. :MFCD09970318
InChI Key :DVRSTRMZTAPMKO-UHFFFAOYSA-N
Pubchem ID :16086114

Safety of AMG-47a

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AMG-47a

RTK

Isoform Comparison

Biological Activity

Description
AMG-47a is a highly potent and orally bioavailable inhibitor of lymphocyte-specific protein tyrosine kinase (Lck), with an exceptionally low IC50 of 0.2 nM. Beyond its primary target, AMG-47a also effectively inhibits several other kinases, including VEGF2, p38α, Jak3, alongside mixed lymphocyte reaction (MLR) and interleukin-2 (IL-2) production, with IC50 values ranging from 1 nM to 72 nM. These properties equip AMG-47a with significant anti-inflammatory capabilities, marking it as a compound of interest for inflammatory disease research and potential therapeutic development[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
A375 cells 1μM 24 hours Evaluate the inhibitory effect of AMG-47a on ERK1/2 phosphorylation PMC6076322
Murine RAW cells 0.25–0.5 µM 24 h AMG-47a inhibited TSI-induced necroptosis at 0.25–0.5 µM but showed toxicity at doses >1 µM. PMC8976052
Murine dermal fibroblasts (MDFs) 1 µM 6 h or 24 h Assessed the ability of AMG-47a to protect against necroptotic cell death induced by TSQ or TSI, showing significant protection against TSQ-induced cell death. PMC8976052
Human THP-1 cells ~100 nM to ~2.5 µM 24 h or 48 h AMG-47a robustly protected THP-1 cells from TSI-induced cell death with IC50 values of ~100 nM to ~2.5 µM. PMC8976052
Human HT29 cells ~100 nM to ~2.5 µM 24 h or 48 h AMG-47a robustly protected HT29 cells from TSQ- and TSI-induced cell death with IC50 values of ~100 nM to ~2.5 µM. PMC8976052
Human U937 cells ~100 nM to ~2.5 µM 24 h or 48 h AMG-47a robustly protected U937 cells from TSQ- and TSI-induced cell death with IC50 values of ~100 nM to ~2.5 µM. PMC8976052
HoxA9-Meis1 AML cells 125 nM to 1 µM 24 h AMG-47a provided substantial protection against necroptotic cell death in HoxA9-Meis1 AML cells at 125 nM to 1 µM. PMC8976052

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.34mL

1.87mL

0.93mL

18.67mL

3.73mL

1.87mL

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