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E-3810

Cat. No. M1936
E-3810 Structure
Synonym:

E3810

Size Price Availability Quantity
5mg USD 210 In stock
10mg USD 345 In stock
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Quality Control
Biological Activity

E-3810 is a novel dual inhibitor of the VEGF and FGF receptors. E-3810 has shown strong antiangiogenic properties as well as outstanding antitumor activity in a large number of preclinical models after oral administration, including resistant settings, and has shown high synergy in combination. E-3810 potently and selectively inhibited VEGF receptor (VEGFR)-1, -2, and -3 and FGF receptor (FGFR)-1 and -2 kinases in the nanomolar range. E-3810 exhibited striking antitumor properties at well-tolerated oral doses administered daily in a variety of tumor xenograft models, including early- or late-stage subcutaneous and orthotopic models. In Matrigel plug assays performed in nude mice, E-3810 inhibited basic FGF-induced angiogenesis and reduced blood vessel density as assessed by histologic analysis. E-3810 reduced the distribution of angiogenesis-sensitive contrast agents after only 5 days of treatment.

Customer Product Validations & Biological Datas
Source Mol Cancer Ther (2013). Figure 5. E-3810
Method Immunohistochemistry
Cell Lines MDA-MB-231 tumor-bearing mice
Concentrations 20 mg/kg
Incubation Time 1, 4, and 24 hours
Results However, the proportion of necrosis was 2 to 20 times higher than in controls in all groups that received active treatments, except for paclitaxel singleagent, with the largest increase in the groups treated with E-3810 alone or in combination
Protocol
Cell Experiment
Cell lines H146 cells
Preparation method Proliferation assay
H146 (2 ~3*103 cells/50 uL/well) in SFM containing 0.5% BSA were cultured in 96-well multi-plates. After overnight culture at 37 C, SFM (150 uL/well) containing 0.5% FBS and several concentrations of SCF were added with or without several concentrations of compound. After culture for 72 hr, the ratios of surviving cells were measured by WST-1.
Concentrations 0~10 μ M
Incubation time 72 h
Animal Experiment
Animal models Female BALB/c nude mice bearing H146 tumorxenograft model
Formulation 0.5% methylcellulose and saline
Dosages 30 and 100 mg/kg twice a day from day 1 to day 21
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 443.49
Formula C26H25N3O4
CAS Number 1058137-23-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models.
Bello E, et al. Cancer Res. 2011 Feb 15;71(4):1396-405. PMID: 21212416.

E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition.
Matsui J, et al. Int J Cancer. 2008 Feb 1;122(3):664-71. PMID: 17943726.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: E-3810, E3810 supplier, VEGFR/PDGFR, inhibitors

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