Lenvatinib Mesylate

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.

Product information

CAS Number: 857890-39-2

Molecular Weight: 522.96

Formula: C22H23ClN4O7S

Synonym:

Lenvima

ER-203492-00

E-7080

Lenvatinib

Lenvatinib mesylate

trade name Lenvima

Chemical Name: 4-(3-chloro-4-(3-cyclopropylureido)phenoxy)-7-methoxyquinoline-6-carboxamide mesylate

Smiles: COC1=CC2=NC=CC(OC3=CC(Cl)=C(C=C3)NC(=O)NC3CC3)=C2C=C1C(N)=O.CS(O)(=O)=O

InChiKey: HWLFIUUAYLEFCT-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

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.

In Vivo:

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.

References:

1. 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.
2. 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.
3. 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.

Products are for research use only. Not for human use.