|
|
| | LDC1267 Basic information |
| Product Name: | LDC1267 | | Synonyms: | LDC1267;N-[4-[(6,7-dimethoxy-4-quinolyl)oxy]-3-fluoro-phenyl]-4-ethoxy-1-(4-fluoro-2-methyl-phenyl)pyrazole-3-carboxamide;N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)-1H-pyrazole-3-carboxamide;CS-1641;LDC 1267;LDC-1267;1H-Pyrazole-3-carboxamide, N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)-;LDC1267 USP/EP/BP;N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluoro-2-methylphenyl)-1H-pyrazole-3-carboxamide | | CAS: | 1361030-48-9 | | MF: | C30H26F2N4O5 | | MW: | 560.55 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1361030-48-9.mol |  |
| | LDC1267 Chemical Properties |
| Boiling point | 628.4±55.0 °C(Predicted) | | density | 1.32±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | insoluble in H2O; insoluble in EtOH; ≥20.75 mg/mL in DMSO | | form | solid | | pka | 9.36±0.70(Predicted) |
| | LDC1267 Usage And Synthesis |
| Biological Activity | LDC1267 is a highly selective TAM kinase inhibitor with IC50s of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Low activity against Met, Aurora B, Lck, Src, and CDK8. | | in vitro | LDC1267 moderately affected proliferation in 11 of 95 different cell lines with IC50 >5 μM. In NKG2D-activated NK cells, it abrogates the inhibitory effect of Gas6 stimulation. | | in vivo | In B16F10 melanoma-bearing mice, LDC1267 (20 mg/kg, ip) potently enhanced anti-metastatic NK cell activity and resisted tumor metabolism without severe cytotoxicity. | | target | | Target | Value | Mer
(Cell-free assay) | <5 nM | Tyro3
(Cell-free assay) | 8 nM | Axl
(Cell-free assay) | 29 nM |
|
| | LDC1267 Preparation Products And Raw materials |
|