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E7820

Cat. No. M9781
E7820 Structure
Synonym:

E-7820

Size Price Availability Quantity
10mg USD 100  USD100 In stock
25mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

E7820 is a α2 integrin inhibitor which suppressing integrin alpha 2, a cell adhesion molecule expressed on endothelial cells. E7820 inhibits proliferation of HUVEC induced by either bFGF and VEGF in serum-free medium with IC50 values of 0.10 and 0.081 μg/mL, respectively.

In vivo, E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg.

Chemical Information
Molecular Weight 336.37
Formula C17H12N4O2S
CAS Number 289483-69-8
Solubility (25°C) DMSO ≥ 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ken Ito, et al. Cancer Sci. Enhanced anti-angiogenic effect of E7820 in combination with erlotinib in epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer xenograft models

[2] Ron J Keizer, et al. AAPS J. Evaluation of α2-integrin expression as a biomarker for tumor growth inhibition for the investigational integrin inhibitor E7820 in preclinical and clinical studies

[3] Taro Semba, et al. Clin Cancer Res. An angiogenesis inhibitor E7820 shows broad-spectrum tumor growth inhibition in a xenograft model: possible value of integrin alpha2 on platelets as a biological marker

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Integrin Binding Peptide

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  Catalog
Abmole Inhibitor Catalog




Keywords: E7820, E-7820 supplier, Integrin, inhibitors, activators


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