Lenvatinib Mesylate, also known as E7080, is a synthetic, orally available inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR/FLK-1) tyrosine kinase with potential antineoplastic activity. E7080 blocks VEGFR2 activation by VEGF, resulting in inhibition of the VEGF receptor signal transduction pathway, decreased vascular endothelial cell migration and proliferation, and vascular endothelial cell apoptosis.
Chemical Formula: C22H23ClN4O7S
Molecular Weight: 522.96
Elemental Analysis: C, 50.53; H, 4.43; Cl, 6.78; N, 10.71; O, 21.42; S, 6.13
trade name Lenvima
InChi Code: InChI=1S/C21H19ClN4O4.CH4O3S/c1-29-19-10-17-13(9-14(19)20(23)27)18(6-7-24-17)30-12-4-5-16(15(22)8-12)26-21(28)25-11-2-3-11;1-5(2,3)4/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28);1H3,(H,2,3,4)
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Lenvatinib mesylate (E7080 mesylate) has IC50s of 4, 5.2, 22 nM for VEGFR2(KDR), VEGFR3(Flt-4), and VEGFR1/Flt-1, respectively. Lenvatinib inhibits PDGFRα, PDGFRβ, FGFR1, and KIT with IC50s of 51, 39, 46, 100 nM, respectively.
Lenvatinib mesylate (E7080 mesylate) (100 mg/kg, p.o.) is administeredand bevacizumab significantly inhibits local tumor growth at the m.f.p., and at the end of treatment, Lenvatinib mesylate also significantly inhibits metastasis to both regional lymph nodes and distant lung.
Lenvatinib mesylate (E7080 mesylate) inhibits the growth of H146 tumor at 30 and 100 mg/kg (BID, QDx21) in a dose-dependent manner and causes tumor regression at 100 mg/kg in H146 xenograft model. IHC analysis with anti-CD31 antibody shows that lenvatinib at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and imatinib treatment.
Sato N, Beppu T, Kinoshita K, Yuki H, Suyama K, Yuruki H, Motohara T, Chiyonaga S, Akahoshi S. Partial Splenic Embolization for Lenvatinib Therapy-associated Thrombocytopenia Among Patients With Hepatocellular Carcinoma. Anticancer Res. 2019 Dec;39(12):6895-6901. doi: 10.21873/anticanres.13909. PubMed PMID: 31810959.
Rinninella E, Cintoni M, Raoul P, Mele MC, De Gaetano AM, Marini MG, Mora V, Gasbarrini A. Minimal impact of lenvatinib (Lenvima®) on muscle mass in advanced hepatocellular carcinoma and implications for treatment duration. Two cases from the REFLECT study. Eur Rev Med Pharmacol Sci. 2019 Nov;23(22):10132-10138. doi: 10.26355/eurrev_201911_19583. PubMed PMID: 31799685.
Feng F, Li X, Li R, Li B. The multiple-kinase inhibitor lenvatinib inhibits the proliferation of acute myeloid leukemia cells. Animal Model Exp Med. 2019 Sep 3;2(3):178-184. doi: 10.1002/ame2.12076. eCollection 2019 Sep. PubMed PMID: 31773093; PubMed Central PMCID: PMC6762047.
Kudo M. A New Treatment Option for Intermediate-Stage Hepatocellular Carcinoma with High Tumor Burden: Initial Lenvatinib Therapy with Subsequent Selective TACE. Liver Cancer. 2019 Oct;8(5):299-311. doi: 10.1159/000502905. Epub 2019 Sep 18. PubMed PMID: 31768341; PubMed Central PMCID: PMC6872999.
Hatanaka T, Kakizaki S, Nagashima T, Namikawa M, Tojima H, Shimada Y, Takizawa D, Naganuma A, Arai H, Sato K, Harimoto N, Shirabe K, Uraoka T. Analyses of objective response rate, progression-free survival, and adverse events in hepatocellular carcinoma patients treated with lenvatinib: A multicenter retrospective study. Hepatol Res. 2019 Nov 23. doi: 10.1111/hepr.13460. [Epub ahead of print] PubMed PMID: 31760660.
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