B-9800 Brigatinib, Free Base, >99%

Solubility: DMSO.

BRG-101

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• Brigatinib, also known as AP26113, inhibited ALK, IGF-1R, and InsR kinases with IC50 values of 0.37 nM, 24.9 nM, and 196 nM, respectively.  It blocked the viability of Karpas 299 cells (ALK+) with an IC50 of 29 nM in vitro.  It demonstrated efficacy in multiple ALK+ xenografts in mice, including Karpas-299 (anaplastic large-cell lymphomas) and H3122 (non-small-cell lung cancer [NSCLC]) xenografts.  Huang W.S., et al. "Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase." J. Med. Chem. 59: 4948-4964 (2016).
• Brigatinib potently inhibited ALK and ROS1 kinases, with a high selectivity over >250 other kinases.  Among a panel of ALK+ cell lines, brigatinib inhibited native ALK (IC50, 10 nmol/L) with 12-fold higher potency than crizotinib.  Excellent efficacy of brigatinib was also observed in mice with ALK+ tumors.  Zhang S., et al. "The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models." Clin. Cancer Res. 22: 5527-5538 (2016).
• For patients with ALK-positive NSCLC who had not previously received an ALK inhibitor, progression-free survival was significantly longer among patients treated with brigatinib than among those treated with crizotinib. Camidge D.R., et al. "Brigatinib versus Crizotinib in ALK-Positive Non-Small-Cell Lung Cancer." N. Engl. J. Med. 379: 2027-2039 (2018).
• Other CAS numbers previously assigned to Brigatinib, Free Base, 1350848-43-9 and 1574359-10-6 have been deleted by CAS and are no longer in use.
• Brigatinib is the active ingredient in the drug product sold under the trade names Alunbrig® and Briganix®.  This drug is currently approved in a least one country for treatment of patients with anaplastic lymphoma kinase -positive metastatic non-small cell lung cancer who have progressed on or are intolerant to crizotinib. NOTE:  THE BRIGATINIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT ALUNBRIG® OR BRIGANIX®, AND IS NOT FOR HUMAN USE.
• 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.