A-2300 Alectinib, Free Base, >99%

Synonyms : [AF802] [CH5424802]

Related Terms : [Alecensa]

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  • 5 mg
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  • 10 mg
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  • 25 mg
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  • 50 mg
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  • 100 mg
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  • 276
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  • 200 mg
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  • 250 mg
  • 585
  • 516
  • 444
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  • 500 mg
  • 997
  • 880
  • 756
  • 109,900
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  • M.W. 482.62
  • C30H34N4O2
  • [1256580-46-7]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO.

  • Alectinib, also known as CH 5424802, is a potent, selective, and orally available ALK inhibitor (IC50 = 1.9 nM) and has weak or no inhibition against 24 other tested protein kinases.  It has selective antitumor activity against cancers with ALK gene alterations, including non-small cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo.  It also blocked ALK L1196M, which corresponds to the gatekeeper mutation giving common resistance to kinase inhibitors, and prevented EML4-ALK L1196M-driven cell growth.  Sakamoto H., et al. "CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant." Cancer Cell 19: 679-690 (2011).
  • Alectinib reduced the tumor size in EML4-ALK-positive xenograft tumors that was not able to regress fully during treatment with crizotinib.  Alectinib also inhibited the growth of some EML4-ALK mutant-driven tumors, such as the G1269A model.  Kodama T., et al. "Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance." Cancer Lett. 351: 215-221 (2014).
  • Two ALK mutations, a V1180L gatekeeper mutation from the cell line model and I1171T mutation from a patient, were found to develop resistance to alectinib and to crizotinib, but were sensitive to ceritinib and other next-generation ALK-TKIs.  Katayama R., et al. "Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib." Clin. Cancer Res. 20: 5686-5696 (2014).
  • This research compound is the free acid form of alectinib; we also offer  the HCl salt form of alectinib; please see Cat. No. A-2311, Alectinib, Hydrochloride Salt.  The free base form of alectinib is used for some or all alectinib formulations for use in humans.
  • Alectinib is the active ingredient in the drug product sold under the trade name Alecensa.  This drug is currently approved in at least one country for use in patients with ALK fusion-gene positive, un-resectable, advanced or recurrent non-small cell lung cancer.   NOTE:  THE ALECTINIB, FREE BASE RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT ALECENSA, AND IS NOT FOR HUMAN USE.
  • Related CAS numbers:   1256589-74-8 for the hydrochloride salt (1:1);  1256590-18-7 for the hydrochloride salt, equivalent ratio not specified; 1358953-69-1 for the methanesulfonate salt, equivalent ratio not specified;  1820744-87-3 for the hydrochloride hydrate salt (1:1:1).
  • Another CAS number previously assigned to Alectinib, namely 1416163-60-4, has been deleted by CAS and is no longer in 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.
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