Caffeic Acid Phenethyl Ester

Catalog No.S7414

Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.

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Caffeic Acid Phenethyl Ester Chemical Structure

Caffeic Acid Phenethyl Ester Chemical Structure
Molecular Weight: 284.31

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Product Information

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Product Description

Biological Activity

Description Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.
Targets NF-κB [1]
In vitro Caffeic acid phenethyl ester blocks NF-κB activation induced by phorbol ester, ceramide, okadaic acid, and hydrogen peroxide by preventing the translocation of the p65 subunit of NF-κB to the nucleus. [1] In a series of tumor cell lines, Caffeic acid phenethyl ester shows promising antiproliferative activity with EC50 of 1.76, 3.16, 13.7, and 44.0 μM against murine colon 26-L5, murine B16-BL6 melanoma, human HT-1080 fibrosarcoma and human lung A549 adenocarcinoma cell lines, respectively. [2] Caffeic acid phenethyl ester, as a potent antioxidant, exerts its anti-apoptotic effect in cerebellar granule cells by blocking ROS formation and inhibiting caspase activity. [3] Moreover, Caffeic acid phenethyl ester attenuates the pro-inflammatory phenotype of LPS-stimulated HSCs, and LPS-induced sensitization of HSCs to fibrogenic cytokines by inhibiting NF-κB signaling. [4]
In vivo In vivo, Caffeic acid phenethyl ester (10 mg/kg, i.p.) inhibits the growth and angiogenesis of primary tumors in C57BL/6 and BALB/c mice inoculated with Lewis lung carcinoma, colon carcinoma, and melanoma cells. [5] Caffeic acid phenethyl ester (5, 10, 20 mg/kg) also shows immunomodulatory effects in vivo by decreasing thymus weight and/or cellularity of thymus and spleen. [6]
Features

Protocol(Only for Reference)

Cell Assay:

[2]

Cell lines Murine colon 26-L5, murine B16-BL6 melanoma, human HT-1080 fibrosarcoma and human lung A549 adenocarcinoma cell lines
Concentrations ~200 μM
Incubation Time 3 days
Method

Human HT-1080 fibrosarcoma, human lung A549 adenocarcinoma and murine B16-BL6 melanoma cell lines are maintained in EMEM medium supplemented with 10% FCS, 0.1% sodium bicarbonate and 2 mM glutamine. Murine colon 26-L5 carcinoma cell line, on the other hand, is maintained in RPMI medium containing the same supplements as in EMEM. These are all highly metastatic cell lines except for A-549 carcinoma. Cellular viability is determined using the standard MTT assay. In brief, exponentially growing cells are harvested and 100 μl of cell suspension containing 2000 cells is plated in 96-well microtiter plates. After 24 h of incubation to allow for cell attachment, the cells are treated with varying concentrations of test samples in medium (100 μl) and incubated for 72 h at 37°C under 5% CO2. Three hours after the addition of MTT, the amount of formazan formed is measured spectrophotometrically at 550 nm with a Perkin Elmer HTS-7000 plate reader. The test samples are first dissolved in DMSO and then diluted with medium; the final concentration of DMSO is less than 0.25%. Normal also had the same extent of DMSO. 5-Fluorouracil (5-FU) and doxorubicin HCl are used as positive controls, and EC50 values are calculated from the mean values of data from 4 wells.

Animal Study:

[5]

Animal Models C57BL/6 and BALB/c mice inoculated with Lewis lung carcinoma, colon carcinoma, and melanoma cells
Formulation PBS
Dosages ~10 mg/kg
Administration i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Natarajan K, et al. Proc Natl Acad Sci U S A. 1996, 93(17), 9090-9095.

[2] Banskota AH, et al. J Ethnopharmacol. 2002, 80(1), 67-73.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02767752 Not yet recruiting Pancreatic Cancer Herlev Hospital|GENIS September 2016 Phase 2
NCT00960544 Not yet recruiting Breast Cancer M.D. Anderson Cancer Center|Myriad Genetic Laboratories,  ...more M.D. Anderson Cancer Center|Myriad Genetic Laboratories, Inc. September 2016 Phase 2
NCT02831179 Not yet recruiting Functional Pancreatic Neuroendocrine Tumor|Malignant Somatostatinoma|Merkel Cell Carcinoma|Metastatic Adrenal Gland Pheochromocytoma|Metastatic Car  ...more Functional Pancreatic Neuroendocrine Tumor|Malignant Somatostatinoma|Merkel Cell Carcinoma|Metastatic Adrenal Gland Pheochromocytoma|Metastatic Carcinoid Tumor|Multiple Endocrine Neoplasia Type 1|Multiple Endocrine Neoplasia Type 2A|Multiple Endocrine Neoplasia Type 2B|Neuroendocrine Neoplasm|Non-Functional Pancreatic Neuroendocrine Tumor|Pancreatic Glucagonoma|Pancreatic Insulinoma|Recurrent Adrenal Cortex Carcinoma|Recurrent Adrenal Gland Pheochromocytoma|Recurrent Merkel Cell Carcinoma|Somatostatin-Producing Neuroendocrine Tumor|Stage III Adrenal Cortex Carcinoma|Stage III Thyroid Gland Medullary Carcinoma|Stage IIIA Merkel Cell Carcinoma|Stage IIIB Merkel Cell Carcinoma|Stage IV Adrenal Cortex Carcinoma|Stage IV Merkel Cell Carcinoma|Stage IVA Thyroid Gland Medullary Carcinoma|Stage IVB Thyroid Gland Medullary Carcinoma|Stage IVC Thyroid Gland Medullary Carcinoma|Thymic Carcinoid Tumor|VIP-Producing Neuroendocrine Tumor|Well Differentiated Adrenal Cortex Carcinoma|Zollinger Ellison Syndrome Vanderbilt-Ingram Cancer Center|National Cancer Institute  ...more Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) August 2016 Phase 1
NCT02795988 Not yet recruiting Gastrointestinal Neoplasms|Adenocarcinoma Imugene Limited August 2016 Phase 1|Phase 2
NCT02574455 Not yet recruiting Breast Cancer Immunomedics, Inc. July 2016 Phase 3

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Chemical Information

Download Caffeic Acid Phenethyl Ester SDF
Molecular Weight (MW) 284.31
Formula

C17H16O4

CAS No. 104594-70-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms CAPE, Phenylethyl Caffeate
Solubility (25°C) * In vitro DMSO 57 mg/mL (200.48 mM)
Ethanol 57 mg/mL (200.48 mM)
Water <1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-Propenoic acid,3-(3,4-dihydroxyphenyl)-, 2-phenylethyl ester

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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