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MTOX1006

Sigma-Aldrich

BCRP/MRP2 Double Knockout Caco-2 Cells

Human male colorectal tissue, adenocarcinoma

Synonym(s):

C2BBe1 Cells BCRP/MRP2 (-/-/-/-,-/-/-/-)

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About This Item

UNSPSC Code:
41106514
NACRES:
NA.81

product name

BCRP/MRP2 Double Knockout Caco-2 Cells, one vial

biological source

human male colorectal tissue (Source disease: adenocarcinoma)

form

liquid

technique(s)

drug transporter assay: suitable
permeability assay: suitable

OMIM accession no.

601107
603756

application(s)

ADME/TOX

storage temp.

−196°C

Gene Information

human ... ABCC2(1244) , ABCG2(9429)

General description

The C2BBe1 cells, a subclone of Caco-2 cells, correspond to ATCC CRL-2102. The BCRP and MRP2 knockout C2BBe1 cells are adenocarcinoma, epithelial cells from a human caucasian male (aged 72 years) with functional double knockout of the ABCG2 and ABCC2 (BCRP/MRP2) efflux transporters.

Application

The following posters and articles demonstrate how Caco-2 cells can be used for cell based assays:

Transporter Function in Caco-2 Cells with Targeted P-Glycoprotein, MRP2 and BCRP Gene Knockout Using Zinc Finger Nucleases

Comparison of Function and Relative Transporter Protein Concentrations in Caco-2 Cells with Single and Double Knockouts of the ABCB1, ABCG2, and ABCC2 Genes

Caco-2 Transporter Knockout Cell Based Assays

Features and Benefits

The Caco-2 subclone C2BBe1 cells are ideal for transporter analysis as they express multiple transporters, are human derived, and grow in a homogenous monolayer that forms tight juntions which is necessary for efflux ratio analysis. Other benefits include:

  • A functional double knockout of the BCRP gene and MRP2 gene eliminates the reliance on chemical inhibitors to determine if a compound is an MDR1 substrate
  • The vial format enables the BCRP and MRP2 knockout cells to be included in standard drug transporter protocols
  • Human assay with no interference from animal inhibitors
  • Overcome the limitations of RNAi and knockdown cell lines that arise from remaining transporter functionality

Legal Information

ADME/Tox Cell Lines License

Disclaimer

RESEARCH USE ONLY. This product is regulated in France when intended to be used for scientific purposes, including for import and export activities (Article L 1211-1 paragraph 2 of the Public Health Code). The purchaser (i.e. enduser) is required to obtain an import authorization from the France Ministry of Research referred in the Article L1245-5-1 II. of Public Health Code. By ordering this product, you are confirming that you have obtained the proper import authorization.

Kit Components Also Available Separately

Product No.
Description
SDS
  • MTOX1006BCRP/MRP2 Double Knockout Caco-2 Cells, one vial 1 vialSDS

Storage Class

10 - Combustible liquids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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P Artursson
Journal of pharmaceutical sciences, 79(6), 476-482 (1990-06-01)
A human intestinal cell line, Caco-2, was used as a model to study the passive diffusion of drugs across intestinal epithelium. The cells formed continuous monolayers when grown on permeable filters of polycarbonate. After 10 days in culture, the monolayers
M J Briske-Anderson et al.
Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.), 214(3), 248-257 (1997-03-01)
The Caco-2 cell line is used by many investigators as a model of the intestinal epithelium to study nutrient uptake and transport. Our goal was to create an awareness of inherent variabilities in the Caco-2 cell line which may influence
Mark I Kaldas et al.
The Journal of pharmacy and pharmacology, 55(3), 307-312 (2003-05-02)
Resveratrol is a dietary constituent suggested to have protective effects against cancer as well as cardiovascular disease. The purpose of the study was to learn whether this agent could be absorbed in man and enter the systemic circulation. This was
S Yee
Pharmaceutical research, 14(6), 763-766 (1997-06-01)
To evaluate and optimize the use of Caco-2 cell monolayers to predict the in vivo absorption of a broad range of compounds in man. Caco-2 cells are derived from human adenocarcinoma colon cells and spontaneously differentiate when grown on porous
V Pade et al.
Journal of pharmaceutical sciences, 87(12), 1604-1607 (1999-04-03)
The objective of this investigation was to establish a relationship between drug permeability and solubility in vitro and the extent of drug absorption in humans. We selected drugs with varying permeabilities and solubilities with the aim of establishing a relationship
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Articles

The Role of Intestinal Efflux Transporters In Drug Absorption

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Drug transport assays in a 96-well system: reproducibility and correlation to human absorption

Application note on Drug transport assays in a 96-well system using Millicell-96 System from Millipore.

Caco-2 Intestinal Drug Transporter Models for More Predictive Drug Absorption

Utilize these Caco-2 cell based assay tools for screening small molecule drug compounds prior to clinical studies and submission to regulatory agencies.

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