Lenvatinib-d4 (E7080-d4) 是氘标记的 Lenvatinib。 Lenvatinib (E7080) 是一种口服的多靶点酪氨酸激酶抑制剂，可抑制 VEGFR1-3、FGFR1-4、PDGFR、KIT 和 RET，显示出有效的抗肿瘤活性。
Lenvatinib-d4 is intended for use as an internal standard for the quantification of lenvatinib by GC- or LC-MS. Lenvatinib is an inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and VEGFR3 (IC50s = 4.0 and 5.2 nM, respectively).1,2 It is slightly less potent against the related kinases VEGFR1, FGFR1, PDGFRα, PDGFRβ, and Kit (IC50s = 22, 46, 51, 39, and 100 nM, respectively).1 Lenvatinib (30 mg/kg, twice per day) reduces tumor growth in an H146 small cell lung cancer mouse xenograft model and induces tumor regression when administered at a dose of 100 mg/kg twice per day. Formulations containing lenvatinib have been used in the treatment of differentiated thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma.
|1. Matsui, J., Yamamaoto, Y., Funahashi, Y., 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(3), 664-671 (2008).|2. Matsui, J., Funahashi, Y., Uenaka, T., et al. Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinase. Clin. Cancer Res. 14(17), 5459-5465 (2008).
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