Cabozantinib | Met and VEGFR2 inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 5 mg | $70.00 | ||
| 25 mg | $230.00 |
Cabozantinib (849217-68-1) is a novel inhibitor of c-met and VEGFR2 kinase activity, IC50=3.5 nm and 35 pM respectively.1 Inhibits MET-activating kinase domain mutations Y1248H, D1246N or K1262R, IC50=3.8, 11.8 and 14.6 nM respectively. In cellular assays it inhibits the following kinases: MET, VEGF2, KIT, FLT3 and AXL, IC50=7.8, 1.9, 5.0, 7.5 and 42 μM respectively.1 Eliminated approximately 80% of vasculature in spontaneous pancreatic islet tumors over 7 days in a mouse model.2 Clinically useful anticancer agent.3
References/Citations:
1) Yakes et al. (2011), Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth; Mol. Cancer Ther., 10 2298
2) You et al. (2011), VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer; Cancer Res., 71 4758
3) Kurzrock et al. (2011), Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor in patients with medullary thyroid cancer; J. Clin. Oncol., 29 2660
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
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Cabozantinib (849217-68-1) is a novel inhibitor of c-met and VEGFR2 kinase activity, IC50=3.5 nm and 35 pM respectively.1 Inhibits MET-activating kinase domain mutations Y1248H, D1246N or K1262R, IC50=3.8, 11.8 and 14.6 nM respectively. In cellular assays it inhibits the following kinases: MET, VEGF2, KIT, FLT3 and AXL, IC50=7.8, 1.9, 5.0, 7.5 and 42 μM respectively.1 Eliminated approximately 80% of vasculature in spontaneous pancreatic islet tumors over 7 days in a mouse model.2 Clinically useful anticancer agent.3
References/Citations:
1) Yakes et al. (2011), Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth; Mol. Cancer Ther., 10 2298
2) You et al. (2011), VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer; Cancer Res., 71 4758
3) Kurzrock et al. (2011), Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor in patients with medullary thyroid cancer; J. Clin. Oncol., 29 2660
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