C-2086 Ceritinib, Free Base, >99%

Synonyms : [LDK-378]

Related Terms : [Zykadia]

  • Size
  • US $
  • £
  • ¥
  • 5 mg
  • 59
  • 50
  • 43
  • 6,500
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  • In stock
  • 10 mg
  • 81
  • 68
  • 59
  • 8,900
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  • In stock
  • 25 mg
  • 133
  • 112
  • 98
  • 14,700
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  • 50 mg
  • 222
  • 188
  • 164
  • 24,500
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  • 100 mg
  • 355
  • 301
  • 262
  • 39,200
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  • 200 mg
  • 533
  • 451
  • 393
  • 58,800
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  • In stock
  • 500 mg
  • 875
  • 742
  • 646
  • 96,500
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  • In stock

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  • M.W. 558.14
  • C28H36ClN5O3S
  • [1032900-25-6]

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  • Ceritinib, also known as LDK-378, is a very selective anaplastic lymphoma kinase (ALK) inhibitor. It inhibits ALK with an IC50 of 200 pM. It inhibits kinases IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively and other kinases tested with IC50s of >100 nM. In vivo it displayed efficacy in anaplastic large cell lymphoma (ALCL) and non-small-cell lung cancer (NSCLC) cancer xenograft models at well-tolerated doses. Marsilje T.H., et al. "Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials." J. Med. Chem. 56: 5675-5690 (2013).
  • Non-small-cell lung cancers (NSCLC) harboring ALK gene rearrangements always develop resistance to the ALK tyrosine kinase inhibitor crizotinib. Ceritinib effectively inhibited crizotinib-resistant ALK with L1196M, G1269A, I1171T and S1206Y mutations. However, ceritinib did not overcome two crizotinib-resistant ALK mutations, G1202R and F1174C. Friboulet L., et al. "The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer." Cancer Discov. 4: 662-673 (2014).
  • A phase 1 clinical trial showed ceritinib was highly active in patients with advanced, ALK-rearranged NSCLC. Certinib was also active in patients who had had disease progression during crizotinib treatment regardless of the presence of resistance mutations in ALK. Shaw A.T., et al. "Ceritinib in ALK-rearranged non-small-cell lung cancer." N. Engl. J. Med. 370: 1189-1197 (2014).
  • Ceritinib is the active ingredient in the drug product sold under the trade name Zykadia®. This drug is currently approved in at least one country for use in patients with ALK-positive metastatic non-small cell lung cancer (NSCLC) following treatment with crizotinib. NOTE: THE CERITINIB, FREE BASE RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT ZYKADIA®, AND IS NOT FOR HUMAN USE.
  • Related CAS numbers: 1380575-43-8 for the dihydrochloride salt.
  • 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.