Lenvatinib Mesylate

Modify Date: 2024-01-02 14:46:47

Lenvatinib Mesylate Structure
Lenvatinib Mesylate structure
 Common Name Lenvatinib Mesylate
CAS Number 857890-39-2 Molecular Weight 522.959
Density N/A Boiling Point N/A
Molecular Formula C22H23ClN4O7S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Lenvatinib Mesylate


Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].

 Names

Name lenvatinib mesylate
Synonym More Synonyms

 Lenvatinib Mesylate Biological Activity

Description Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
Related Catalog
Target

VEGFR1:22 nM (IC50)

VEGFR2:4 nM (IC50)

VEGFR3:5.2 nM (IC50)

FGFR1:46 nM (IC50)

FGFR2

FGFR3

FGFR4

PDGFRα:51 nM (IC50)

PDGFRβ:39 nM (IC50)

c-Kit:100 nM (IC50)

RET

In Vitro Lenvatinib mesylate (E7080 mesylate) 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, 100 nM, respectively[3].
In Vivo Lenvatinib mesylate (E7080 mesylate) (100 mg/kg, p.o.) is administeredand bevacizumab 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[3]. Lenvatinib mesylate (E7080 mesylate) 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 imatinib treatment[4].
References

[1]. Kudo M, et al. Lenvatinib versus sorafenib in first-line treatment of patients with unresectable hepatocellularcarcinoma: a randomised phase 3 non-inferiority trial. Lancet. 2018 Mar 24;391(10126):1163-1173.

[2]. Suyama K, et al. Lenvatinib: A Promising Molecular Targeted Agent for Multiple Cancers. Cancer Control. 2018 Jan-Dec;25(1):1073274818789361.

[3]. 3.Matsui J, et al. 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. Clin Cancer Res. 2008, 14(17),545.

[4]. Matsui J, et al. 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. Int J Cancer. 2008, 122(3), 664-671.

 Chemical & Physical Properties

Molecular Formula C22H23ClN4O7S
Molecular Weight 522.959
Exact Mass 522.097595
PSA 182.80000
LogP 5.81830

 Synthetic Route

Lenvatinib (E7080) structure

Lenvatinib (E7080)

CAS#:417716-92-8

Methanesulfonic acid structure

Methanesulfonic acid

CAS#:75-75-2

~%

Lenvatinib Mesylate Structure

Lenvatinib Mesylate

CAS#:857890-39-2

Literature: Eisai Co., Ltd. Patent: EP1698623 A1, 2006 ; Location in patent: Page/Page column 17 ;

 Synonyms

4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide mesylate
Lenvatinib mesilate
lenvatinib mesylate
Lenvatinib mesylate [USAN]
4-{3-Chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxy-6-quinolinecarboxamide methanesulfonate (1:1)
4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate
4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxyquinoline-6-carboxamide,methanesulfonic acid
6-Quinolinecarboxamide, 4-[3-chloro-4-[[(cyclopropylamino)carbonyl]amino]phenoxy]-7-methoxy-, methanesulfonate (1:1)
Lenvatinib mesilate (JAN)
lenvatinib methanesulfonate
UNII-3J78384F61
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Related Compounds: More...
Lenvatinib (E7080)
417716-92-8
Lenvatinib Impurity 7
417714-14-8
Lenvatinib Impurity 6
417717-21-6
Lenvatinib Impurity 5
417717-20-5
6-Carbamoyl-4-(3-chloro-4-(3-cyclopropylureido)phenoxy)-7-methoxyquinoline 1-oXnde
1788901-86-9
Lenvatinib Impurity 2
2380197-90-8
Eprosartan mesylate
144143-96-4
TVP1022 (mesylate)
202464-88-8
BPR1R024 mesylate
2763365-40-6
4-((Cyclohexylamino)methyl)benzoic acid hydrochloride
1158522-08-7
1-[(2,4-Dichlorophenyl)methyl]-N-(1,1-dimethylethyl)-2-methyl-1H-indole-3-methanamine
940364-43-2
2-(Azidomethyl)-5-(4-methylphenyl)furan
2228586-92-1
2-Methoxy-6-(pyrazol-1-yl)-benzonitrile
134104-43-1
1H-3-Benzazepin-7-ol, 8-chloro-2,3,4,5-tetrahydro-5-(3-iodophenyl)-3-methyl-, (S)-
131615-57-1
(4-Methyl-tetrahydro-furan-2-yl)-methanol
6906-52-1
N-(1-cyanocyclopentyl)-2-[4-(4-fluorobenzenesulfonyl)-1,4-diazepan-1-yl]acetamide
930439-75-1
4,5,6,7-Tetrahydrobenzo[d]isoxazole-3-carbaldehyde
1018584-77-4
tert-Butyl-DL-alanine
1375289-11-4
5-Bromo-2-(chloromethyl)-1H-imidazole
2169055-08-5
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