1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    FGFR
    PDGFR
    c-Kit
    RET
  3. Lenvatinib

Lenvatinib (Synonyms: E7080)

Cat. No.: HY-10981 Purity: 99.74%
Handling Instructions

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

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 84 In-stock
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50 mg USD 180 In-stock
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100 mg USD 228 In-stock
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200 mg USD 348 In-stock
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500 mg USD 648 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target[1][2][3]

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 (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[3].

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[3].
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[4].

Clinical Trial
Molecular Weight

426.85

Formula

C₂₁H₁₉ClN₄O₄

CAS No.

417716-92-8

SMILES

O=C(N)C1=C(C=C2N=CC=C(C2=C1)OC3=CC=C(C(Cl)=C3)NC(NC4CC4)=O)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 37.5 mg/mL (87.85 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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]

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 STI571, and VEGF neutralization antibody are suspended in 0.5% methylcellulose and saline, respectively, and administered orally twice a day for lenvatinib and STI571 and twice a week for antibody from day 1 to day 21. Tumor volume is measured on the indicated days and calculated. 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

Purity: 99.74%

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Lenvatinib
Cat. No.:
HY-10981
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