E7820 (Synonyms: ER68203-00) |
カタログ番号GC19128
One-Click Copy Product Info
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E7820 (ER68203-00) は、経口で活性な芳香族スルホンアミド誘導体であり、内皮上のインテグリン α2 サブユニットの発現を抑制する独自の血管新生阻害剤です。 E7820 は、ラット大動脈の血管新生を 0.11 μg/ml の IC50 で阻害します。 E7820 は、α-1、α-2、α-3、および α-5 インテグリン mRNA 発現を調節します。抗血管新生および抗腫瘍活性。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 289483-69-8
Sample solution is provided at 25 µL, 10mM.
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E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
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 ug/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 ug/mL, respectively[3].
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].
References:
[1]. Ito K, et al. 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. Cancer Sci. 2014 Aug;105(8):1023-31.
[2]. Keizer RJ, et al. Evaluation of α2-integrin expression as a biomarker for tumor growth inhibition for the investigational integrin inhibitor E7820 in preclinical and clinical studies. AAPS J. 2011 Jun;13(2):230-9.
[3]. Semba T, et al. 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. Clin Cancer Res. 2004 Feb 15;10(4):1430-8.
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Cell experiment: |
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. |
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Animal experiment: |
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. |
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References: [1]. Ito K, et al. 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. Cancer Sci. 2014 Aug;105(8):1023-31. |
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| Cas No. | 289483-69-8 | SDF | |
| 同義語 | ER68203-00 | ||
| Canonical SMILES | O=S(C1=CC(C#N)=CC=C1)(NC2=C(NC=C3C#N)C3=C(C)C=C2)=O | ||
| Formula | C17H12N4O2S | M.Wt | 336.37 |
| 溶解度 | DMSO : ≥ 33 mg/mL (98.11 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9729 mL | 14.8646 mL | 29.7292 mL |
| 5 mM | 594.6 μL | 2.9729 mL | 5.9458 mL |
| 10 mM | 297.3 μL | 1.4865 mL | 2.9729 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)