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  3. E7820

E7820 (Synonyms: ER68203-00)

Cat. No.: HY-14571 Purity: 99.36%
Handling Instructions

E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.

For research use only. We do not sell to patients.

E7820 Chemical Structure

E7820 Chemical Structure

CAS No. : 289483-69-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 97 In-stock
Estimated Time of Arrival: December 31
5 mg USD 88 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 315 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity[1][2].

In Vitro

E7820 (ER68203-00) inhibits both bFGF- and VEGF-driven ube formation of human umbilical vascular endothelial cell (HUVEC) in a dose-dependent manner with IC50 of 0.20 and 0.24 μg/ml, respectively[1].
E7820 inhibits proliferation of HUVEC induced by either bFGF or VEGF in serum-free medium (SFM). The IC50 values are 0.10 and 0.081 μg/ml, respectively. Antiproliferative activity of E7820 against both WiDr and LoVo cells is very weak compared with that against HUVEC. The values of IC50 were 29 and 15 μg/ml, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

E7820 (ER68203-00) (50-200 mg/kg; p.o. ; twice daily for 14 days) delays the growth of WiDr cells inoculated s.c.[1].
E7820 (200-400 mg/kg; p.o.;once daily for 4 days) potently inhibits WiDr-induced angiogenesis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old female nude mice (KSN mice, WiDr-induced angiogenesis model) [1]
Dosage: 50, 100, 200 mg/kg
Administration: p.o. ; twice daily for 14 days from 2 days after inoculation of the tumor cells
Result: The antitumor effect was dose-dependent at 50, 100, and 200 mg/kg, and the tumor growth rates were 52%, 46%, and 27%, respectively.
Clinical Trial
Molecular Weight

336.37

Formula

C₁₇H₁₂N₄O₂S

CAS No.

289483-69-8

SMILES

O=S(C1=CC(C#N)=CC=C1)(NC2=C(NC=C3C#N)C3=C(C)C=C2)=O

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 : 100 mg/mL (297.29 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9729 mL 14.8646 mL 29.7292 mL
5 mM 0.5946 mL 2.9729 mL 5.9458 mL
10 mM 0.2973 mL 1.4865 mL 2.9729 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 (7.43 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.36%

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Keywords:

E7820ER68203-00E 7820E-7820IntegrinHUVECsulfonamidederivativeendotheliumcolorectaltumorcellWiDrLoVoInhibitorinhibitorinhibit

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E7820
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