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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

Essai

≥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.
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.

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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Certificats d'analyse (COA)

Lot/Batch Number
0000221887
0000221889
0000220386
0000238353
0000188187

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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
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
Guoqing Tang et al.
Journal of molecular neuroscience : MN, 70(9), 1437-1444 (2020-05-10)
The therapeutic effect of deferoxamine (DFO) for spinal cord injury (SCI) has been demonstrated in previous studies; however, the exact mechanism of action is still unclear. Here, we hypothesized that DFO ameliorates spinal cord compression by promoting neovascularization. Using an
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
Taku Shigesawa et al.
Carcinogenesis, 42(1), 58-69 (2020-05-26)
In hepatocellular carcinoma (HCC), a subset of cells defined by high CD44 and CD133 expression has been reported to possess cancer stem-like cell (CSC) characteristics and to be associated with a poor prognosis. Since the approval of the multikinase inhibitor
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