| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T33990 | ||||
| Target Name | Macrophage colony-stimulating factor 1 (CSF1) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | ABT-869 | Drug Info | IC50 = 3 nM | [2] | |
| Axitinib | Drug Info | IC50 = 16 nM | [2] | ||
| Action against Disease Model | Axitinib | Drug Info | Axitinib inhibits cellular autophosphorylation of VEGF receptors (VEGFR) with picomolar IC(50) values. Counterscreening across multiple kinase and protein panels shows it is selective for VEGFRs. Axitinib blocks VEGF-mediated endothelial cell survival, tube formation, and downstream signaling through endothelial nitric oxide synthase, Akt and extracellular signal-regulated kinase. | [1] | |
| References | |||||
| REF 1 | Intravesically administered antisense oligonucleotides targeting heat-shock protein-27 inhibit the growth of non-muscle-invasive bladder cancer. BJU Int. 2008 Aug 5;102(5):610-6. | ||||
| REF 2 | Colony-stimulating factor-1 receptor inhibitors for the treatment of cancer and inflammatory disease. Curr Top Med Chem. 2009;9(7):599-610. | ||||
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