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Lenvatinib

CAT: 0013-GTR19162245-02Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19162245-02Size:500 mg
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Description
Lenvatinib (E7080) is a multitargeted kinase inhibitor with IC50s of 4/5.2/22/46 nM for VEGFR2/VEGFR3/VEGFR1/FGFR1 in cell free assays; also inhibits PDGFR, Kit with IC50< 100 nM; suppresses the phosphorylation of VEGF receptor-2 and FGF receptor 1 and inhibits proliferation of endothelial cellin vitro; orally active.Kidney Cancer Approved (In Vitro) :Lenvatinib (E7080) 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, and 100 nM, respectively. (In Vivo) :Lenvatinib (E7080) (100 mg/kg, p.o.) 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 (E7080) 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 STI571 treatment.
CAS Number
417716-92-8
Product Name Alternative
E7080 | E-7080 | E 7080
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
COC1=CC2=NC=CC (OC3=CC (Cl) =C (NC (=O) NC4CC4) C=C3) =C2C=C1C (N) =O
Molecular Formula
C21H19ClN4O4
Molecular Weight
426.853
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
6-Quinolinecarboxamide, 4-[3-chloro-4-[[ (cyclopropylamino) carbonyl]amino]phenoxy]-7-methoxy-

Chemical Information

Lenvatinib

Lenvatinib is a member of the class of quinolines that is the carboxamide of 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxylic acid. A multi-kinase inhibitor and orphan drug used (as its mesylate salt) for the treatment of various types of thyroid cancer that do not respond to radioiodine. It has a role as an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, a fibroblast growth factor receptor antagonist, a vascular endothelial growth factor receptor antagonist and an orphan drug. It is a member of phenylureas, a member of quinolines, a monocarboxylic acid amide, an aromatic ether, a member of cyclopropanes, an aromatic amide and a member of monochlorobenzenes. It is a conjugate base of a lenvatinib(1+).

CAS Number417716-92-8
PubChem CID9823820
IUPAC Name4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxyquinoline-6-carboxamide
Molecular FormulaC21H19ClN4O4
Molecular Weight426.9
XLogP2.8
Topological Polar Surface Area116
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count5
Rotatable Bond Count6
Heavy Atom Count30
Formal Charge0
Complexity634
SMILES
COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl
InChI
InChI=1S/C21H19ClN4O4/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/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28)
InChIKey
WOSKHXYHFSIKNG-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Lenvatinib
CAS: 417716-92-8
CID: 9823820
Formula: C21H19ClN4O4
MW: 426.9
Interactive 3D Structure
Loading 3D structure...
Computed Properties
PropertyValue
Molecular Weight426.9
XLogP32.8
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count5
Rotatable Bond Count6
Exact Mass426.1094828
Monoisotopic Mass426.1094828
Topological Polar Surface Area116 Ų
Heavy Atom Count30
Formal Charge0
Complexity634
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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