MedChemExpress LLC (MCE)

MedChemExpress - Model Cabozantinib - 849217-68-1

Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1][2].

Cabozantinib

MCE China：Cabozantinib

Brand：MedChemExpress (MCE)

Cat. No.HY-13016

CAS：849217-68-1

Synonyms：XL184; BMS-907351

Purity：99.96%

Storage：4°C, protect from light *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.

In Vitro：Cabozantinib 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[1]. Cabozantinib (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[1]. Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion[1]. Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types[1].

In Vivo：Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice[1]. Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis[1]. Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner[1].

IC50 & Target：VEGFR2 0.035 nM (IC50) Axl Flt-4 6 nM (IC50) Flt-1 12 nM (IC50) Met 1.3 ± 1.2 nM (IC50)

References：

[1]. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308. [Content Brief]

[2]. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768. [Content Brief]

[3]. Fuse MA, et al. Combination Therapy With c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. Mol Cancer Ther. Mol Cancer Ther. 2017 Nov;16(11):2387-2398. [Content Brief]

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