Repositioning Candidate Details
| Candidate ID: | R0920 |
| Source ID: | DB06080 |
| Source Type: | investigational |
| Compound Type: | small molecule |
| Compound Name: | Linifanib |
| Synonyms: | ABT-869; Linifanib |
| Molecular Formula: | C21H18FN5O |
| SMILES: | CC1=CC(NC(=O)NC2=CC=C(C=C2)C2=C3C(N)=NNC3=CC=C2)=C(F)C=C1 |
| Structure: |
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| DrugBank Description: | Linifanib (ABT-869) is a small molecule vascular endothelial growth factor (VEGF) receptor-based kinase inhibitor that is designed to suppress tumor growth by preventing the formation of new blood vessels that supply the tumor with oxygen and nutrients and by inhibiting key angiogenic signaling pathways. Linifanib is intended for the treatment of hematologic malignancies and the solid tumors. |
| CAS Number: | 796967-16-3 |
| Molecular Weight: | 375.407 |
| DrugBank Indication: | Investigated for use/treatment in leukemia (myeloid), myelodysplastic syndrome, and solid tumors. |
| DrugBank Pharmacology: | ABT-869 was effective in a broad range of cancers including small cell lung carcinoma, colon carcinoma, breast carcinoma and MV4-11 tumors in vitro and in vivo. ABT-869 induced significant apoptosis in cells with FLT3 mutation in vitro (IC50 value of 4 nM) and profound anti-leukemic effect in a mouse xenograft model. However, in vitro ABT-869 only shows minimal cytotoxic effect on AML cells with wild-type FLT3. Based on the preclinical studies suggesting the role of VEGF pathways in leukemogenesis, it is likely that the anti-leukemic effect of ABT-869 will be best evaluated in vivo. |
| DrugBank MoA: | ABT-869, a multi-targeted receptor tyrosine kinase inhibitor, has been shown to inhibit of all members of the VEGF and PDGF receptor families (e.g., KDR IC50 value of 4 nM), and have less activity (IC50 values >1 µM) against unrelated receptor tyrosine kinases, soluble tyrosine kinases and serine/threonine kinases. In addition, it exhibits potent anti-proliferative and apoptotic effects on tumor cells dependent on mutant, constitutively active, FLT3 and KIT kinases. |
| Targets: | Receptor-type tyrosine-protein kinase FLT3; Vascular endothelial growth factor receptor 1; Vascular endothelial growth factor receptor 2; Vascular endothelial growth factor receptor 3; Mast/stem cell growth factor receptor Kit; Macrophage colony-stimulating factor 1 receptor |
| Inclusion Criteria: | Therapeutic strategy associated |
