Cabozantinib, S-Malate Salt (BMS-907351, Cometriq, XL-184, CAS 849217-68-1), >99%

LC Laboratories' Product Number C-8999 - Cabozantinib, S-Malate Salt (BMS-907351, Cometriq, XL-184, CAS 849217-68-1), >99% - for research use only. 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 µM, respectively. Cabozantinib inhibited tumor angiogenesis, tumor growth and metastasis in cancers with dysregulated MET and VEGFR signaling. This research compound is the S-malate salt form of cabozantinib. We also offer the free base form; please see Cabozantinib, Free Base, Cat. No. C-8901. 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. Cabozantinib is active in patients with medullary thyroid cancer and has an acceptable safety profile. 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. Cabozantinib demonstrated activity in patients with metastatic melanoma in a phase 2 randomized discontinuation trial. Cabozantinib was active in patients with metastatic non-small cell lung cancer (NSCLC) in a phase 2 randomized discontinuation trial. 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 S-malate salt, whose CAS number is given above. The CAS number of the free base form is 849217-68-1. Another CAS number previously assigned to cabozantinib S-malate, namely 942407-59-2, has been deleted by CAS and is no longer in use.LC Laboratories' Product Number C-8999 - Cabozantinib, S-Malate Salt (BMS-907351, Cometriq, XL-184, CAS 849217-68-1), >99% - for research use only. 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 µM, respectively. Cabozantinib inhibited tumor angiogenesis, tumor growth and metastasis in cancers with dysregulated MET and VEGFR signaling. This research compound is the S-malate salt form of cabozantinib. We also offer the free base form; please see Cabozantinib, Free Base, Cat. No. C-8901. 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. Cabozantinib is active in patients with medullary thyroid cancer and has an acceptable safety profile. 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. Cabozantinib demonstrated activity in patients with metastatic melanoma in a phase 2 randomized discontinuation trial. Cabozantinib was active in patients with metastatic non-small cell lung cancer (NSCLC) in a phase 2 randomized discontinuation trial. 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 S-malate salt, whose CAS number is given above. The CAS number of the free base form is 849217-68-1. Another CAS number previously assigned to cabozantinib S-malate, namely 942407-59-2, has been deleted by CAS and is no longer in use.

• Supplier: LC Laboratories
• Product #: C-8999
• Sku #: C-8999_100mg