1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Lenvatinib (Synonyms: E7080)

Cat. No.: HY-10981 Purity: 99.69%
Data Sheet SDS Handling Instructions

Lenvatinib is an orally active, multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, and less potent against VEGFR1/Flt-1, and appr 10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β.

For research use only. We do not sell to patients.
Lenvatinib Chemical Structure

Lenvatinib Chemical Structure

CAS No. : 417716-92-8

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10 mM * 1 mL in DMSO $55 In-stock
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10 mg $70 In-stock
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Lenvatinib is an orally active, multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, and less potent against VEGFR1/Flt-1, and appr 10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β.

IC50 & Target

IC50: 4 nM (VEGFR2), 5.2 nM (VEGFR3)

In Vitro

Lenvatinib inhibits KIT kinase with an IC50 value of 100 nM. lenvatinib inhibits SCF- and VEGF-induced tube formation in a dose-dependent manner with IC50 values of 5.2 and 5.1 nM, respectively. Lenvatinib inhibits SCF-induced proliferation of another human SCLC, H526 cells, which expresses KIT, at the concentrations required for the inhibition of KIT kinase. The IC50 values of Lenvatinib against phosphorylation of KDR and KIT in HUVEC are about 500 times lower than those against H146 proliferation in vitro[1]. Lenvatinib inhibits both angiogenesis and lymphangiogenesis induced by human breast cancer cells, and significantly inhibits tumor growth of MDA-MB-231. Lenvatinib and bevacizumab treatment decreases MVD by almost the same extent[2]. Lenvatinib inhibits proliferation at high concentrations (mean IC50s 23.6-44.17 μM) in the majority of the cell lines, while the IC50 in the KM12C colon cancer cell line is 9.54 μM[3].

In Vivo

Lenvatinib 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[1]. lenvatinib (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 also significantly inhibits metastasis to both regional lymph nodes and distant lung[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00280397 Eisai Inc. Cancer: Solid Tumors January 2006 Phase 1
NCT01728623 Eisai Co., Ltd.|Eisai Inc. Thyroid Cancer September 2012 Phase 2
NCT00784303 Eisai Inc. Thyroid Cancer August 2009 Phase 2
NCT00946153 Eisai Co., Ltd.|Eisai Inc. Hepatocellular Carcinoma July 2009 Phase 1|Phase 2
NCT00832819 Eisai Co., Ltd.|Eisai Inc. Non-small-cell Lung Cancer February 2009 Phase 1
NCT00121680 Eisai Inc. Metastatic Melanoma July 2005 Phase 1
NCT01268293 Eisai Co., Ltd.|Eisai Inc. Cancer February 2011 Phase 1
NCT02915172 M.D. Anderson Cancer Center|Eisai Inc. Advanced Cancer|Malignant Neoplasm of Breast|Malignant Neoplasms of Bone and Articular Cartilage|Malignant Neoplasms of Digestive Organs|Malignant Neoplasms of Eye Brain and Other Parts of Central Nervous System|Malignant Neoplasms of Female Genital Organs|Malignant Neoplasms of Ill-defined Secondary and Unspecified Sites|Malignant Neoplasms of Independent (Primary) Multiple Sites|Malignant Neoplasms of Lip Oral Cavity and Pharynx|Malignant Neoplasms of Male Genital Organs|Malignant Neoplasms of December 2016 Phase 1
NCT02640508 Virginia G. Kaklamani|Eisai Inc.|The University of Texas Health Science Center at San Antonio Cancer|Solid Tumor May 2016 Phase 2
NCT02860936 Fondazione IRCCS Istituto Nazionale dei Tumori, Milano Adenoid Cystic Carcinomas of the Salivary Glands June 2015 Phase 2
NCT02657369 Eisai Inc. Thyroid Cancer, Anaplastic July 7, 2016 Phase 2
NCT02199379 Eisai Inc. Renal Impairment|Disease Severity November 2011 Phase 1
NCT02846766 Teresa Helsten, MD|Eisai Co., Ltd.|University of California, San Diego Cancer June 2016 Phase 2
NCT02454478 Eisai Co., Ltd.|Eisai Inc. Carcinoma, Renal Cell July 2015 Phase 1
NCT02788708 Floor Backes|Eisai Inc.|Ohio State University Comprehensive Cancer Center Fallopian Tube Carcinoma|Recurrent Ovarian Cancer|Primary Peritoneal Carcinoma|Recurrent Endometrial Cancer May 27, 2016 Phase 1
NCT03006887 Eisai Co., Ltd.|Eisai Inc. Solid Tumors January 19, 2017 Phase 1
NCT01111461 Eisai Inc. Endometrial Cancer March 2010 Phase 2
NCT01321554 Eisai Inc. Thyroid Cancer March 17, 2011 Phase 3
NCT01133977 Eisai Inc.|Quintiles, Inc. Stage IV Melanoma April 2010 Phase 1|Phase 2
NCT02702388 Eisai Inc. Thyroid Cancer March 28, 2016 Phase 2
NCT02501096 Eisai Inc. Tumors July 22, 2015 Phase 1|Phase 2
NCT03168074 National University Hospital, Singapore|Eisai Co., Ltd.|Tan Tock Seng Hospital Breast Cancer March 28, 2017 Phase 2
NCT03009292 Eisai Inc. Solid Tumor January 2019 Phase 1
NCT03006926 Eisai Co., Ltd.|Eisai Inc. Hepatocellular Carcinoma February 28, 2017 Phase 1
NCT02199392 Eisai Inc. P-glycoprotein|Healthy Volunteers November 2011 Phase 1
NCT02780310 Memorial Sloan Kettering Cancer Center|Eisai Inc. Adenoid Cystic Carcinoma May 19, 2016 Phase 2
NCT01877083 Eisai Co., Ltd.|Eisai Inc. KIF5B-RET-Positive Adenocarcinoma of the Lung April 2013 Phase 2
NCT02686164 Eisai Inc. Tumors May 12, 2016 Phase 1
NCT02579616 Eisai Co., Ltd.|Eisai Inc. Biliary Tract Cancer October 2015 Phase 2
NCT02578316 Eisai Inc. Advanced Solid Tumors|Lymphomas June 2009 Phase 1
NCT02953743 Eisai Co., Ltd.|Eisai Inc. Unresectable Hepatocellular Carcinoma (HCC) August 2016 Phase 1
NCT01136967 Eisai Inc. Unresectable Stage III|Stage IV Melanoma August 2010 Phase 2
NCT02966093 Eisai Co., Ltd.|Eisai Inc. Differentiated Thyroid Cancer (DTC) February 7, 2017 Phase 3
NCT02792829 Eisai Inc. Healthy Volunteers August 2014 Phase 1
NCT01761266 Eisai Limited|Eisai Inc. Hepatocellular Carcinoma (HCC) March 14, 2013 Phase 3
NCT03173560 Eisai Inc. Renal Cell Carcinoma May 31, 2017 Phase 2
NCT02421042 Eisai Inc. Hepatic Impairment|Hepatic Function June 2011 Phase 1
NCT02562118 National University Hospital, Singapore|Eisai Co., Ltd. Breast Cancer September 2015 Phase 1|Phase 2
NCT01525394 Eisai Inc. Refractory Solid Tumors|Lymphomas December 2010 Phase 1
NCT00121719 Eisai Inc. Solid Tumor or Lymphoma July 2005 Phase 1
NCT02723630 Eisai Inc. Healthy Volunteers July 2013 Phase 1
NCT02726503 Translational Research Informatics Center, Kobe, Hyogo, Japan Anaplastic Thyroid Cancer April 4, 2016 Phase 2
NCT01529112 Eisai Inc.|Quintiles, Inc. Non-Small Cell Lung Cancer November 2011 Phase 2
NCT03008369 Mayo Clinic|National Cancer Institute (NCI) Malignant Adrenal Gland Pheochromocytoma|Malignant Paraganglioma|Metastatic Adrenal Gland Pheochromocytoma July 2017 Phase 2
NCT02211222 Eisai Inc. Differentiated Thyroid Cancer
NCT02430714 Eisai Co., Ltd.|Eisai Inc. Thyroid Neoplasms May 20, 2015
NCT02678780 Grupo Espanol de Tumores Neuroendocrinos|Eisai Limited|Experior S.L. Neuroendocrine Tumors October 2015 Phase 2
NCT02973997 Academic and Community Cancer Research United|National Cancer Institute (NCI) Columnar Cell Variant Thyroid Gland Papillary Carcinoma|Follicular Variant Thyroid Gland Papillary Carcinoma|Poorly Differentiated Thyroid Gland Carcinoma|Recurrent Thyroid Gland Carcinoma|Stage III Differentiated Thyroid Gland Carcinoma|Stage III Thyroid Gland Follicular Carcinoma|Stage III Thyroid Gland Papillary Carcinoma|Stage IV Thyroid Gland Follicular Carcinoma|Stage IV Thyroid Gland Papillary Carcinoma|Stage IVA Differentiated Thyroid Gland Carcinoma|Stage IVA Thyroid Gland Follicular Ca April 2017 Phase 2
NCT02915783 Eisai Inc. Non Clear Cell Renal Cell Carcinoma (nccRCC) February 20, 2017 Phase 2
NCT03005015 European Organisation for Research and Treatment of Cancer - EORTC Endometrial Neoplasms January 2017 Phase 2
NCT02432274 Eisai Limited|Eisai Inc. Tumors|Solid Malignant Tumors|Osteosarcoma|Differentiated Thyroid Cancer (DTC) December 29, 2014 Phase 1|Phase 2
NCT02935309 H. Lee Moffitt Cancer Center and Research Institute Rectal Cancer|Rectal Adenocarcinoma October 11, 2016 Phase 1
NCT01136733 Eisai Inc. Metastatic Renal Cell Carcinoma August 2010 Phase 1|Phase 2
NCT01133756 Eisai Inc.|PharmaBio Development Inc. Ovarian Cancer March 2010 Phase 1|Phase 2
NCT02811861 Eisai Inc. Renal Cell Carcinoma October 13, 2016 Phase 3
NCT01137604 Eisai Inc. Glioma November 2010 Phase 2
NCT03139747 Abramson Cancer Center of the University of Pennsylvania Thyroid Cancer April 3, 2017 Phase 2
NCT01433991 Eisai Inc. Advanced Solid Tumors October 2011 Phase 1|Phase 2
NCT02592356 M.D. Anderson Cancer Center Advanced Cancers|Endocrine Tumor November 2015
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.3427 mL 11.7137 mL 23.4274 mL
5 mM 0.4685 mL 2.3427 mL 4.6855 mL
10 mM 0.2343 mL 1.1714 mL 2.3427 mL
Kinase Assay
[1]

Tyrosine kinase assays are performed by HTRF (KDR, VEGFR1, FGFR1, c-Met, EGFR) and ELISA (PDGFRβ), using the recombinant kinase domains of receptors. In both assays, 4 μL of serial dilutions of lenvatinib are mixed in a 96-well round plate with 10 μL of enzyme, 16 μL of poly (GT) solution (250 ng) and 10 μL of ATP solution (1 μM ATP) (final concentration of DMSO is 0.1%). In wells for blanks, no enzyme is added. In control wells no test article is added. The kinase reaction is initiated by adding ATP solution to each well. After 30-min incubation at 30°C, the reaction is stopped by adding 0.5mol/LEDTA (10 μL/well) to the reaction mixture in each well. Dilution buffer adequate to each kinase assay is added to the reaction mixture. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Lenvatinib is dissolved in SFM containing 0.5% FBS and several concentrations of SCF.

H146 (1.2×103 cells/50 μL/well) in SFM containing 0.5% BSA are cultured in 96-well multi-plates. After overnight culture at 37°C, SFM (150 μL/well) containing 0.5% FBS and several concentrations of SCF are added with or without several concentrations of compound. After culture for 72 hr, the ratios of surviving cells are measured by WST-1. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Lenvatinib is suspended in 0.5% methylcellulose.

Female BALB/c nude mice (8-12 weeks old, 20-25 g) are maintained under clean-room conditions. H146 tumor cells (6.5×106) are implanted subcutaneously (s.c.) into the flank region of mice. Twelve days after inoculation, mice are randomized into control (n=12) and treatment (n=6 or n=5) groups and this point in time is identified as day 1. Lenvatinib and Imatinib, and VEGF neutralization antibody are suspended in 0.5% methylcellulose and saline, respectively, and administered orally twice a day for lenvatinib and imatinib and twice a week for antibody from day 1 to day 21. Tumor volume is measured on the indicated days and calculated according to the following equation: tumor volume (mm3)=length × (width)2/2. Antitumor activity is shown as a relative tumor volume (RTV=calculated tumor volume at indicated days/volume on day 1). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

426.85

Formula

C₂₁H₁₉ClN₄O₄

CAS No.

417716-92-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Lenvatinib
Cat. No.:
HY-10981
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