CAS 857890-39-2|Lenvatinib Mesylate

Introduction：Basic information about CAS 857890-39-2|Lenvatinib Mesylate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Lenvatinib Mesylate BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

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

Names

Name	lenvatinib mesylate
Synonym	More Synonyms

Lenvatinib Mesylate BiologicalActivity

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	Research Areas >>CancerSignaling Pathways >>Protein Tyrosine Kinase/RTK >>PDGFRSignaling Pathways >>Protein Tyrosine Kinase/RTK >>FGFRSignaling Pathways >>Protein Tyrosine Kinase/RTK >>VEGFRSignaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Kit
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
InChIKey	HWLFIUUAYLEFCT-UHFFFAOYSA-N
SMILES	COc1cc2nccc(Oc3ccc(NC(=O)NC4CC4)c(Cl)c3)c2cc1C(N)=O.CS(=O)(=O)O

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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