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SML3017

Lenvatinib mesylate

Name: Lenvatinib mesylate
Brand: SIGMA

≥98% (HPLC), TK inhibitor, powder

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

NACRES:

NA.77

UNSPSC Code:

12352200

MDL number:

MFCD18633219

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Product Name

Lenvatinib mesylate, ≥98% (HPLC)

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

Related Categories

Bioactive Small Molecules

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.

Orally active receptor tyrosine kinase inhibitor against VEGFR (Flt-1/KDR/Flt-4), PDGFR1/2, FGFR1 and KIT with anti- angiogenesis efficacy in vitro and in vivo.

pictograms

GHS08

signalword

Warning

hcodes

H361d,H373

pcodes

P202 - P260 - P280 - P308 + P313 - P405 - P501

Hazard Classifications

Repr. 2 - STOT RE 2

target_organs

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

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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Non‑invasive monitoring of paclitaxel and lenvatinib efficacy against anaplastic thyroid cancer in orthotopic SCID mouse models using small‑animal FDG‑PET/CT.

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

Different Mechanisms of Action of Regorafenib and Lenvatinib on Toll-Like Receptor-Signaling Pathways in Human Hepatoma Cell Lines.

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

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.

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

Dual Vascular Endothelial Growth Factor Receptor and Fibroblast Growth Factor Receptor Inhibition Elicits Antitumor Immunity and Enhances Programmed Cell Death-1 Checkpoint Blockade in Hepatocellular Carcinoma.

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

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.