SML3017

Lenvatinib mesylate

≥98% (HPLC)

• 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
• Empirical Formula (Hill Notation): C₂₁H₁₉ClN₄O₄ · CH₄O₃S
• CAS Number: 857890-39-2
• Molecular Weight: 522.96
• MDL number: MFCD18633219
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• 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

Description

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.

Safety Information

• 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