| 生物活性 | Cabozantinib hydrochloride is a potent and orally active inhibitor ofVEGFR2andMET, withIC50values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition ofKIT,RET,AXL,TIE2, andFLT3(IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cellapoptosis[1]. |
体外研究
(In Vitro) | Cabozantinib hydrochloride inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively[1].
Cabozantinib hydrochloride (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively[1].
Cabozantinib hydrochloride (0-370 nM, 24 h) inhibits cellular migration and invasion[1].
Cabozantinib hydrochloride (48 h) inhibits tumor cell proliferation in a variety of tumor types[1].
Cell Proliferation Assay | Cell Line: | SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells[1] | | Concentration: | | | Incubation Time: | 48 hours | | Result: | Inhibited tumor cell proliferation, with IC50of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively. |
Cell Migration Assay | Cell Line: | B16F10 cells[1] | | Concentration: | 0, 41, 123, and 370 nM | | Incubation Time: | 24 hours | | Result: | Potently inhibited HGF-induced migration (IC50= 31 nM) of B16F10 cells. |
Cell Invasion Assay | Cell Line: | B16F10 cells[1] | | Concentration: | 0, 1.5, 14, and 123 nM | | Incubation Time: | 24 hours | | Result: | Potently inhibited HGF-induced invasion (IC50= 9 nM) of B16F10 cells. |
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体内研究
(In Vivo) | Cabozantinib hydrochloride (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice[1].
Cabozantinib hydrochloride (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis[1].
Cabozantinib hydrochloride (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner[1].
| Animal Model: | Female mice bearing MBA-MB-231 tumor (5 per group)[1] | | Dosage: | 0, 100 mg/kg | | Administration: | Orally, once | | Result: | Inhibited MET and VEGFR2 phosphorylation. |
| Animal Model: | Mice bearing MBA-MB-231 tumor[1] | | Dosage: | 1, 3, 10, 30, 60 mg/kg | | Administration: | Orally, once daily for 14 days | | Result: | Inhibited tumor growth in a dose-dependent manner. |
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