| Name | Chiauranib |
| Description | Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM. |
| In vitro | In HUVEC and PDGFRβ phosphorylation in PDGFRβ overexpressed NIH3T3 cells, Chiauranib (CS2164; 0.03-3 μM) suppressed VEGFR/PDGFR phosphorylation, inhibited ligand-dependent cell proliferation, and capillary tube formation, and prevented vasculature formation in tumor tissues. Chiauranib (CS2164) inhibited CSF-1R phosphorylation that lead to the suppression of ligand-stimulated monocyte-to-macrophage differentiation and reduced CSF-1R+ cells in tumor tissues. Chiauranib (3 μM; 24 hours) showed induction of G2/M cell cycle arrest and suppression of cell proliferation in tumor tissues through the inhibition of Aurora B-mediated H3 phosphorylation[1]. |
| In vivo | Chiauranib exhibited broad and potent anti-tumor activities in vivo. Chiauranib (2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg; oral) induced remarkable regression or complete inhibition of tumor growth at well-tolerated oral doses in several human tumor xenograft models[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 60 mg/mL (137.78 mM), Sonication is recommended.
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| Keywords | CSF-1R | VEGFR2 | CSF1R | Vascular endothelial growth factor receptor | VEGFR3 | anti-angiogenesis | CD117 | Aurora Kinase | c-Kit | CS-2164 | CSF-1 receptor | colony stimulating factor 1 receptor | PDGFRα | PDGFR | Aurora-B | anticancer | inhibit | SCFR | Inhibitor | VEGFR | Chiauranib | Platelet-derived growth factor receptor | CS 2164 | VEGFR1 | c-Fms |
| Inhibitors Related | Sorafenib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
United States
