Description
AMG-47a is a potent inhibitor of Lck and T cell proliferation. It exhibits anti-inflammatory activity (ED₅₀ = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice. In several other in vitro assays, AMG-47 displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 µM, AMG-47 effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 µM.
AMG-47a is a potent inhibitor of Lck and T cell proliferation. It exhibits anti-inflammatory activity (ED₅₀ =11 mg/kg) in the anti-CD3 induced production of IL-2 in mice. In several other in vitro assays, AMG-47 displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 µM, AMG-47 effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 µM.
Alternate Name/Synonyms: 4-Methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]benzamide
Appearance: Beige solid
Formulation: N/A
CAS Number: 882663-88-9
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₂₉H₂₈F₃N₅O₂
Molecular Weight: 535.56
Cell-Permeable?: yes
Purity: ≥98% by HPLC
Solubilities: DMSO
Handling: Protect from air and light
Country of Origin: USA
Tag Line: AMG-47a is a potent inhibitor of Lck and T cell proliferation
MDL Number: N/A
PubChem CID: 16086114
SMILES: CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)C3=CC4=CN=C(N=C4C=C3)NCCN5CCOCC5
InChi: InChI=1S/C29H28F3N5O2/c1-19-5-6-21(27(38)35-24-4-2-3-23(17-24)29(30,31)32)16-25(19)20-7-8-26-22(15-20)18-34-28(36-26)33-9-10-37-11-13-39-14-12-37/h2-8,15-18H,9-14H2,1H3,(H,35,38)(H,33,34,36)
InChi Key: DVRSTRMZTAPMKO-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |