B-2332 Binimetinib, Free Base, >99%

Solubility: Soluble in DMSO.

BNM-101

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• Binimetinib, also known as MEK162, is a novel, second generation MEK1/2 inhibitor. N-RAS mutant melanoma cultures appeared to be particularly sensitive to binimetinib, which reduced ERK1/2 phosphorylation, induced apoptosis, and significantly reduced clonogenic survival. Thumar, J. et al., "MEK targeting in N-RAS mutated metastatic melanoma." Mol. Cancer 13: 45 (2014).
• Binimetinib induced transient retinopathy with multiple bilateral lesions in some patients with metastatic melanoma. Urner-Bloch, U. et al., "Transient MEK inhibitor-associated retinopathy in metastatic melanoma." Ann. Oncol. 25: 1437-1441 (2014).
• Binimetinib showed some activities in patients with advanced melanoma harboring NRAS or Val600 BRAF mutations in a open-label, non-randomised, phase 2 study. Ascierto, P.A. et al., "MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study." Lancet Oncol. 14: 249-256 (2013).
• Other CAS numbers previously assigned to binimetinib, free base, namely 1073666-70-2, 1201685-05-3, and 1417448-81-7, have been deleted by CAS and are no longer in use.
• Binimetinib is the active ingredient in the drug sold under the trade name Mektovi®. This drug is currently approved in at least one country for use, in combination with encorafenib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. NOTE: THE BINIMETINIB FREE BASE COMPOUND SOLD BY LC LABORATORIES FOR RESEARCH IS NOT MEKTOVI® AND IS NOT SOLD 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.