Product Details
| Alternate Name | 4-Methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]benzamide |
|---|---|
| Appearance | Beige solid |
| CAS # | 882663-88-9 |
| Molecular Formula | C₂₉H₂₈F₃N₅O₂ |
| Molecular Weight | 535.56 |
| Purity | ≥98% by HPLC |
| Solubility | DMSO |
| 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 |
| PubChem CID | 16086114 |
| Handling | Protect from air and light |
| Storage Conditions | -20°C |
| Shipping Conditions | Gel Pack |
| USAGE | For Research Use Only! Not For Use in Humans. |
Details
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.
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