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SML3017

Sigma-Aldrich

Lenvatinib mesylate

≥98% (HPLC)

Synonym(s):

4-[3-Chloro-4-(N’-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, 4-[3-Chloro-4-[(cyclopropylaminocarbonyl)amino]phenoxy]-7-methoxy-6-quinolinecarboxamide mesylate, 4-[3-chloro-4-[[(cyclopropylamino)carbonyl]amino]phenoxy]-7-methoxy-6-Quinolinecarboxamide methanesulfonate (1:1), E 7080 mesylate, E-7080 mesylate, E7080 mesylate, ER-203492-00 mesylate, Lenvatinib methanesulfonate

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About This Item

Empirical Formula (Hill Notation):
C21H19ClN4O4 · CH4O3S
CAS Number:
857890-39-2
Molecular Weight:
522.96
MDL number:
MFCD18633219
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C(C1=CC2=C(OC3=CC=C(C(Cl)=C3)NC(NC4CC4)=O)C=CN=C2C=C1OC)N.O=S(O)(C)=O

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)

InChI key

HWLFIUUAYLEFCT-UHFFFAOYSA-N

Biochem/physiol Actions

Lenvatinib (E7080) is an orally active inhibitor against multiple receptor tyrosine kinases, including VEGFR (Flt-1/KDR/Flt-4 IC50 = 22/4.0/5.2 nM), PDGFR1/2 (IC50 = 39/51 nM), FGFR1 and KIT (IC50 = 46 and 100 nM, respectively) that inhibits angiogenesis in vitro (VEGF/SCF-induced HUVEC tube formation IC50 = 5.1/5.2 nM). Lenvatinib oral administration results in tumor growth arrest (30 mg/kg b.i.d. p.o.) and even regression (100 mg/kg b.i.d. p.o.) in vivo among mice harboring SCF-producing human small cell lung carcinoma H146 cells.

Pictograms

Health hazard
GHS08

Signal Word

Warning

Hazard Statements

H361d,H373

Hazard Classifications

Repr. 2 - STOT RE 2

Target Organs

Gastro-intestinal system,Kidney,Bone,Reproductive organs,Adrenal gland

Storage Class Code

11 - Combustible Solids

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Combining anti-angiogenic therapy with immune checkpoint blockade with anti-programmed cell death-1 (PD-1) antibodies is a promising treatment for hepatocellular carcinoma (HCC). Tyrosine kinase inhibitors are well-known anti-angiogenic agents and offer potential for combination with anti-PD-1 antibodies. This study investigated the
Junji Matsui et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 14(17), 5459-5465 (2008-09-04)
Vascular endothelial growth factor (VEGF)-C/VEGF-receptor 3 (VEGF-R3) signal plays a significant role in lymphangiogenesis and tumor metastasis based on its effects on lymphatic vessels. However, little is known about the effect of inhibiting VEGF-R3 on lymphangiogenesis and lymph node metastases
Junji Matsui et al.
International journal of cancer, 122(3), 664-671 (2007-10-19)
E7080 is an orally active inhibitor of multiple receptor tyrosine kinases including VEGF, FGF and SCF receptors. In this study, we show the inhibitory activity of E7080 against SCF-induced angiogenesis in vitro and tumor growth of SCF-producing human small cell
Reina Sasaki et al.
International journal of molecular sciences, 21(9) (2020-05-14)
Multiple kinase inhibitors are available for patients with advanced hepatocellular carcinoma (HCC). It is largely unknown whether regorafenib or lenvatinib modulates innate immunity including Toll-like receptor (TLR)-signaling pathways in HCC. We performed real-time RT-PCR to investigate 84 TLR-associated gene expression
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Anaplastic thyroid carcinoma (ATC) is a rare type of thyroid carcinoma with a poor prognosis. Thus, suitable preclinical tumor models are required for the development of new ATC therapies. In the present study, orthotopic tumor xenograft models were established using
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