• Cabozantinib, also known as XL184, is an orally bioavailable novel tysosine kinase inhibitor of c-MET and VEGF receptor 2 (VEGFR2). It inhibited MET and VEGFR2 with IC50 values of 1.3 nM and 35 pM, respectively. It also inhibited MET-activating kinase domain mutations Y1248H, D1246N, or K1262R with IC50 values of 3.8, 11.8, and 14.6 nM, respectively. It strongly inhibited several kinases that are implicated in tumor pathobiology including KIT, RET, AXL, TIE2, and FLT3 with IC50 values of 4.6, 5.2, 7, 14.3, and 11.3 nM, respectively. In cellular assays, cabozantinib inhibited phosphorylation of MET, VEGFR2, KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 [micro]M, respectively. Cabozantinib inhibited tumor angiogenesis, tumor growth and metastasis in cancers with dysregulated MET and VEGFR signaling. Yakes F.M., et al \"Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.\" Mol. Cancer Ther. 10: 2298-2308 (2011).
• This research compound is the free base form of cabozantinib. We also offer the s-malate salt form; please see Cabozantinib, s-Malate, Cat. No. C-8999
• Treatment of RIP-Tag2 mice with cabozantinib eliminated approximately 80% of the vasculature of spontaneous pancreatic islet tumors over 7 days, reduced pericytes and empty basement membrane sleeves, resulted in widespread intratumoral hypoxia and tumor cell apoptosis, and delayed regrowth of the tumor vasculature after drug withdrawal. Importantly, it also inhibited invasiveness of primary tumors and reduced metastasis. You W.K., et al. \"VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer.\" Cancer Res. 71: 4758-4768 (2011).
• Cabozantinib is active in patients with medullary thyroid cancer and has an acceptable safety profile. Kurzrock R., et al. \"Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer.\" J. Clin. Oncol. 29: 2660-2666 (2011).
• Cabozantinib 40 mg daily was associated with a high rate of bone scan response and better tolerability in patients with metastatic castration-resistant prostate cancer when compared with previously reported results for cabozantinib 100 mg daily. Lee R.J., et al. \"A dose-ranging study of cabozantinib in men with castration-resistant prostate cancer and bone metastases.\" Clin Cancer Res. 19: 3088-3094 (2013).
• Cabozantinib demonstrated activity in patients with metastatic melanoma in a phase 2 randomized discontinuation trial. Gordon M.S. etal. \"Activity of Cabozantinib (XL184) in Metastatic Melanoma: Results From a Phase 2 Randomized Discontinuation Trial (RDT).\" http://www.exelixis.com/sites/default/files/2012-06-02_Gordon%20Melanoma_ASCO%202012%20FINAL_poster_8531.pdf
• Cabozantinib was active in patients with metastatic non-small cell lung cancer (NSCLC) in a phase 2 randomized discontinuation trial. Hellerstedt B.A. et al. \"Activity of Cabozantinib (XL184) in Metastatic NSCLC: Results From a Phase 2 Randomized Discontinuation Trial (RDT).\" http://www.exelixis.com/sites/default/files/2012-06-05_Hellerstedt%20NSCLC_ASCO%202012_FINAL_poster_7514.pdf
• Cabozantinib is the active ingredient in the drug product sold under the trade name Cometriq®. This drug is currently approved in at least one country for use in patients with medullary thyroid cancer. It is currently undergoing clinical trials for the treatment of prostate, ovarian, brain, melanoma, breast, non-small cell lung, pancreatic, hepatocellular and kidney cancers. NOTE: THE CABOZANTINIB, FREE BASE RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT THE COMETRIQ®, AND IS NOT FOR HUMAN USE.
• This cabozantinib product is the free base, whose CAS number is given above. The CAS number of the s-Malate salt form is 1140909-48-3.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.

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