L-5400 Lenvatinib, Free Base, >99%

Synonyms : [E7080] [ER20349200]

Related Terms : [Lenvima]

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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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  • 200 mg
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  • 250 mg
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  • 500 mg
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  • 1 g
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  • M.W. 426.85
  • C21H19ClN4O4
  • [417716-92-8]

Solubility: Soluble in DMSO.

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  • Lenvatinib, also known as E7080, is an active inhibitor of multiple receptor tyrosine kinases, with IC50 values of 22 nM (VEGFR1), 4 nM (VEGFR2), 5.2 nM (VEGFR3), 46 nM (FGFR1), 51 nM (PDGFRa), 39 nM (PDGFRb), and 100 nM (KIT). It inhibited SCF- and VEGF-induced angiogenesis of human umbilical vein endothelial cells that express the SCF receptor KIT, with IC50 values of 5.2 nM and 5.1 nM, respectively. Lenvatinib inhibited tumor growth in the human small cell lung cancer H146 xenograft model. Matsui J., et al. "E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition." Int. J. Cancer 122: 664-671 (2008).
  • This research compound is the free base form of lenvatinib. We also plan to offer the methanesulfonate salt form; please see Cat. No. L-5433, Lenvatinib, Methanesulfonate Salt. The methanesulfonate salt form will be added to our website as soon as the first lot is ready for shipment.
  • The maximum tolerated dose (MTD) for lenvatinib with carboplatin/paclitaxel is 4 mg BID in advanced non-small cell lung cancer patients. Lenvatinib at the MTD demonstrated tolerability and encouraging antitumor activity. Nishio M., et al. "Phase 1 study of lenvatinib combined with carboplatin and paclitaxel in patients with non-small-cell lung cancer." Br. J. Cancer 109: 538-544 (2013).
  • Lenvatinib had manageable toxicity and showed preliminary activity for durable disease control. The antiangiogenic activity of lenvatinib might be correlated with its antitumor activity in patients with a wide range of solid tumors. Yamada K., et al. "Phase I dose-escalation study and biomarker analysis of E7080 in patients with advanced solid tumors." Clin. Cancer Res. 17: 2528-2537 (2011).
  • Lenvatinib is the active ingredient in the drug product sold under the trade name Lenvima®. This drug is currently approved in at least one country for use in patients with progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer (DTC). NOTE: THE LENVATINIB, FREE BASE RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT LENVIMA®, AND IS NOT FOR HUMAN USE.
  • This lenvatinib product is the free base, whose CAS number is given above. The CAS number of the methanesulfonate salt form is 857890-39-2.
  • Related CAS numbers: 857890-39-2 for the methanesulfonate salt; 857890-31-4 for the hydrochloride (1:1) salt; 857890-35-8 for the toluenesulfonate (1:1) salt; 857890-37-0 for the sulfate (1:1) salt; 857890-41-6 for a methanesulfonate (1:1) hydrate salt whose hydration level was not specified); and 1808104-66-6 for the maleate (1:1) salt.
  • Another CAS number previously assigned to lenvatinib, namely 942407-57-0, 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.