Cabozantinib/[email protected]

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Cabozantinib (Marketed under the tradename Cometriq, formerly known as XL184) is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and has been shown to reduce tumor growth, metastasis, and angiogenesis.

XL184 (Cabozantinib) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM. XL-184 also displays potent activity against Met, Ret, Kit, FLT1, FLT3, FLT4, Tie2, and AXL. XL184 at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion.

Cabozantinib, also known as XL-184 or BMS-907351, is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several tyrosine receptor kinases. Specifically, cabozantinib appears to have a strong affinity for the hepatocyte growth factor receptor (Met) and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in inhibition of tumor growth and angiogenesis, and tumor regression.

XL184 is a pan tyrosine kinase inhibitor that primarily targets VEGFR2 (IC50 = 0.035 nM) and c-Met (IC50 = 1.3 nM) but also inhibits RET, c-Kit, Axl, FLT3, and Tie2 (IC50s = 5.2, 4.6, 7, 11.3, and 14.3 nM, respectively).1 In in vivo breast, lung, and glioma tumor models that represent dysregulated c-Met and VEGFR signaling, XL184 was shown to reduce tumor and endothelial cell proliferation, inhibiting both angiogenesis and metastasis.1 XL184 has undergone clinical trial in a broad number of cancers, including thyroid carcinoma, prostate cancer, ovarian cancer, melanoma, breast cancer, non-small cell lung cancer, hepatocellular cancer, renal cell carcinoma, and glioblastoma.