产品
编 号：F741286
分子式：C28H25ClFN3O5
分子量：537.97
分子式：C28H25ClFN3O5
分子量：537.97
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CAS No: 1817759-42-4
产品详情
生物活性：
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (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 cell apoptosis.
体内研究：
Cabozantinib hydrochloride (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice.Cabozantinib hydrochloride (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis.Cabozantinib hydrochloride (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner.Animal Model:Female mice bearing MBA-MB-231 tumor (5 per group)
Dosage:0, 100 mg/kg
Administration:Orally, once
Result:Inhibited MET and VEGFR2 phosphorylation.
Animal Model:Mice bearing MBA-MB-231 tumor
Dosage:1, 3, 10, 30, 60 mg/kg
Administration:Orally, once daily for 14 days
Result:Inhibited tumor growth in a dose-dependent manner.
体外研究：
Cabozantinib hydrochloride inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively.Cabozantinib hydrochloride (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively.Cabozantinib hydrochloride (0-370 nM, 24 h) inhibits cellular migration and invasion.Cabozantinib hydrochloride (48 h) inhibits tumor cell proliferation in a variety of tumor types.
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (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 cell apoptosis.
体内研究：
Cabozantinib hydrochloride (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice.Cabozantinib hydrochloride (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis.Cabozantinib hydrochloride (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner.Animal Model:Female mice bearing MBA-MB-231 tumor (5 per group)
Dosage:0, 100 mg/kg
Administration:Orally, once
Result:Inhibited MET and VEGFR2 phosphorylation.
Animal Model:Mice bearing MBA-MB-231 tumor
Dosage:1, 3, 10, 30, 60 mg/kg
Administration:Orally, once daily for 14 days
Result:Inhibited tumor growth in a dose-dependent manner.
体外研究：
Cabozantinib hydrochloride inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively.Cabozantinib hydrochloride (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively.Cabozantinib hydrochloride (0-370 nM, 24 h) inhibits cellular migration and invasion.Cabozantinib hydrochloride (48 h) inhibits tumor cell proliferation in a variety of tumor types.
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