cabozantinib
1,1-Cyclopropanedicarboxamide,N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-
CAS: 849217-68-1
Molecular Formula: C28H24FN3O5
cabozantinib - Names and Identifiers
cabozantinib - Physico-chemical Properties
| Molecular Formula | C28H24FN3O5 |
| Molar Mass | 501.51 |
| Density | 1.396 |
| Melting Point | 212-215°C |
| Boling Point | 758.1±60.0 °C(Predicted) |
| Solubility | Soluble in DMSO |
| Appearance | White powder. |
| Color | White |
| pKa | 13.86±0.70(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Use | A potent VEGFR2 and Met inhibitor |
| In vitro study | XL184 is a small molecule inhibitor of multiple receptor tyrosine kinases, particularly c-Met and VEGFR2. XL-184 also effectively acts on Ret, Kit, FLT1, FLT3, FLT4, Tie2, and AXL, with IC50 of 4 nM, 4.6 nM, 12 nM, 11.3 nM, 6 nM, 14.3 nM, and 7 nM. XL184 weakly inhibited RON and PDGFR-β with IC50 of 124 nM and 234 nM, respectively, while it had almost no inhibitory activity on FGFR1 with IC50 of 5.294 μm. Treatment of MPNST cells with XL184 at low concentrations (0.1-0.5 μm) also significantly inhibited constitutive and inducible Met phosphorylation and its downstream signals, and inhibited HGF-induced MPNST cell migration and invasion. XL184 also significantly inhibited Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although the concentration of XL184 at 0.1 μm did not inhibit the growth of MPNST cells, the concentration of 5-10 μm significantly inhibited the growth of MPNST cells. |
| In vivo study | XL184 treated RIP-Tag2 mice bearing spontaneous islet cell tumors at a dose of 30 mg/kg disrupted 83% of tumor blood vessels, reduced pericytes and empty basement membrane sleeves, and caused extensive intratumoral hypoxia and extensive tumor cell apoptosis, moreover, it delays the regrowth of tumor blood vessels after drug withdrawal. Compared with XL999, it significantly inhibits VEGFR rather than c-Met, resulting in a 43% reduction in blood vessels, indicating that VEGFR is inhibited, inhibition also amplifies other functionally related receptor tyrosine kinases (RTKs) that inhibit angiogenesis. XL184 also reduces primary tumor invasion and reduces metastasis. Treatment of SCID mice with XL184 at a dose of 30 mg/kg per day significantly abolished the growth and metastasis of human MPNST xenografts. XL184 treatment of breast cancer, lung cancer glioma model, inhibit tumor growth, this effect is dose-dependent, reduce tumor and endothelial cell proliferation, promote apoptosis. XL184 sustained inhibition of tumor growth in mice bearing MDA-MB-231 tumors and rats bearing C6 tumors at doses of 100 mg/kg and 10 mg/kg, respectively. |
cabozantinib - Reference
| Reference Show more | 1. [IF=3.411] Kui Ling et al."High-Throughput Screen of Natural Compounds and Biomarkers for NSCLC Treatment by Differential Expression and Weighted Gene Coexpression Network Analysis (WGCNA)."Biomed Res Int. 2021;2021:5955343 |
cabozantinib - Introduction
Cabozantinib (XL184, BMS-907351) is an effective VEGFR2 inhibitor. When targeting VEGFR2 and c-Met, IC50 is 0.035 nM, and it also effectively inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2 and AXL,IC50 is 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
Last Update：2022-10-16 17:29:20
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