VEGFR inhibitor
CAS：417716-92-8
分子式：C21H19ClN4O4
分子量：426.85
纯度：98%
存储：Store at -20°C

Background:

Lenvatinib (E7080) is an inhibitor of multiple RTK with IC50 values of 22nM, 4nM, 5.2nM, 39nM and 35nM on VEGFR-1, VEGFR-2, VEGFR-3, PDGFRβ and RET, respectively [1].

Lenvatinib is presently under investigation both as monotherapy and in combination with cytotoxic agents for multiple types of solid tumor, including thyroid carcinoma and hepatocellular carcinoma (in Phase III trials), and melanoma, renal carcinoma, non-small cell lung carcinoma, glioblastoma multiforme, and ovarian and endometrial carcinoma (Phase I and II trials) [1].

When used as an inhibitor of RET kinase, Lenvatinib cause growth inhibition in TPC-1 cells and LC-2/ad cells. The GI50 values are 27nM and 48nM. It is also reported that Lenvatinib can inhibit RET (rearranged during transfection) gene fusion kinases, and inhibit oncogenic signaling of RET gene fusions. Lenvatinib has been demonstrated to exert antitumor activities in RET gene fusion-driven tumor models [2].

参考文献:
[1] Neda Stjepanovic, Jaume Capdevila. Multikinase inhibitors in the treatment

of thyroid cancer: specific role of lenvatinib. Biologics: Targets and Therapy. 2014 (8): 129-139.

[2] Kiyoshi Okamoto, Kotaro Kodama, Kazuma Takase, Naoko Hata Sugi, Yuji Yamamoto, Masao Iwata, Akihiko Tsuruoka. Antitumor activities of the targeted multi-tyrosine kinase inhibitor lenvatinib (E7080) against RET gene fusion-driven tumor models. Cancer Letters. 2013 July（340）：97-103.