A-2300 Alectinib, Free Base, >99%

Synonyms : [AF802] [CH5424802]

Related Terms : [Alecensa]

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  • 25 mg
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  • 50 mg
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  • 100 mg
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  • 200 mg
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  • 250 mg
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  • 500 mg
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  • 1 g
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  • 2 g
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  • 5 g
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  • M.W. 482.62
  • C30H34N4O2
  • [1256580-46-7]

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

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  • 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.
  • 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.
  • 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 SOLD BY LC LABORATORIES FOR RESEARCH IS NOT ALECENSA®, 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.
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