B-2332 Binimetinib, Free Base, >99%

Synonyms : [ARRY438162] [ARRY-162] [MEK162]

Related Terms : [Mektovi]

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  • 25 mg
  • 49
  • 41
  • 35
  • 5,300
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  • 50 mg
  • 72
  • 60
  • 51
  • 7,900
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  • 100 mg
  • 112
  • 94
  • 80
  • 12,200
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  • 200 mg
  • 189
  • 159
  • 135
  • 20,600
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  • 500 mg
  • 339
  • 285
  • 243
  • 37,000
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  • 1 g
  • 641
  • 540
  • 460
  • 69,900
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  • M.W. 441.23
  • C17H15BrF2N4O3
  • [606143-89-9]

Solubility: Soluble in DMSO.

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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 product 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.  NOTE: THE BINIMETINIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT MEKTOVI®, 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.
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