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SML3017

Sigma-Aldrich

Lenvatinib mesylate

≥98% (HPLC)

Synonyme(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

Formule empirique (notation de Hill):
C21H19ClN4O4 · CH4O3S
Numéro CAS:
857890-39-2
Poids moléculaire :
522.96
Numéro MDL:
MFCD18633219
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

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)

Clé InChI

HWLFIUUAYLEFCT-UHFFFAOYSA-N

Actions biochimiques/physiologiques

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.

Pictogrammes

Health hazard
GHS08

Mention d'avertissement

Warning

Mentions de danger

H361d,H373

Classification des risques

Repr. 2 - STOT RE 2

Organes cibles

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

Code de la classe de stockage

11 - Combustible Solids

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Haijing Deng et al.
Liver cancer, 9(3), 338-357 (2020-07-11)
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
Mariko Aoyama et al.
Oncology reports, 44(4), 1709-1716 (2020-09-19)
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
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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