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LDC1267
- Development stage
- Preclinical
- Lead developer
- Qurient
- Modality
- Small Molecules
- Administration
- Oral, Intraperitoneal
01
Overview
LDC1267 is a highly selective, cell-permeable, tight-binding "type II" TAM (Tyro3, Axl, and Mer) receptor tyrosine kinase inhibitor. It exhibits potent inhibitory activity against Mer, Tyro3, and Axl with IC50 values of <5 nM, 8 nM, and 29 nM, respectively, while displaying lower activity against other kinases such as Met, Aurora B, Lck, Src, and CDK8. Developed by the Lead Discovery Center and the Max Planck Society, LDC1267 has been shown to enhance the anti-metastatic activity of natural killer (NK) cells in vivo by blocking the TAM receptor/Cbl-b pathway. It has demonstrated preclinical efficacy in reducing metastases in murine models of breast cancer and melanoma, and is also being investigated for its effects on bone marrow stromal cell senescence and osteoblastic differentiation.
- Other names
- N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-4-ethoxy-1-(4-fluoro-2-methylphenyl)-1H-pyrazole-3-carboxamide
02
Targets
MERTK (MER proto-oncogene, tyrosine kinase)AXL (AXL receptor tyrosine kinase)
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