1. Cytoskeleton
  2. Integrin

E7820 (Synonyms: ER68203-00)

Cat. No.: HY-14571 Purity: 98.62%
Handling Instructions

E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.

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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
25 mg USD 468 In-stock
Estimated Time of Arrival: December 31
50 mg USD 840 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.

In Vitro

E7820 treatment 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. E7820 also inhibits both bFGF- and VEGF-driven tube formation of HUVEC in this assay. The IC50 values are 0.20 and 0.24 μg/mL, respectively[3].

In Vivo

E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models without severe body weight loss. E7820 (50 mg/kg) and erlotinib decrease MVD and enhance apoptosis in tumor-associated endothelial cells, inhibit tumor cell proliferation and enhanced apoptosis, and enhance inhibition of cell proliferation and apoptosis through activation of both intrinsic and extrinsic apoptosis pathways in human NSCLC xenograft models[1]. E7820 shows anti-tumor activity at doses of 50, 100, and 200 mg/kg in the tumor growth and α2-integrin expression experiments[2]. 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[3].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (98.11 mM)

*"≥" means soluble, but saturation unknown.

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.
References
Cell Assay
[3]

Tumor cells are plated at 1 to 2×105 cells/well on 96-well plates in 0.1 mL of RPMI 1640 containing 10% fetal bovine serum. After 24 h, either E7820 or vehicle is added to duplicate cultures of cells, and at 2 or 3 days after addition of E7820, the ratios of surviving cells are measured by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. All experiments are done at least in duplicate and repeated twice.

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

Animal Administration
[1]

A549, H1975, and H1650 cells are s.c. inoculated into 9-week-old female nude mice. Approximately 10 days after inoculation, E7820 (25 and 50 mg/kg) is given orally twice daily and erlotinib (60 mg/kg) is given orally once a day for 3 weeks. Tumor volume (TV) and relative TV (RTV) are calculated by using a formula described previously. The combination effect on RTV is analyzed by using two-way anova.

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

References
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

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

Purity: 98.62%

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Product Name:
E7820
Cat. No.:
HY-14571
Quantity:

E7820

Cat. No.: HY-14571