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MTOX1002P24

Sigma-Aldrich

BCRP Knockout Caco-2 Cells

human cervix, Epithelial

Synonym(s):

BCRP Knockout C2BBe1 Cells

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About This Item

UNSPSC Code:
41106514
NACRES:
NA.81

product name

BCRP Knockout Caco-2 Cells, one assay ready, 24 well plate

biological source

human colon

form

solid

morphology

Epthelial

technique(s)

drug transporter assay: suitable
permeability assay: suitable

application(s)

ADME/TOX

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General description

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

The three week production lead time begins on the Monday following a purchase, in the third week the plates are shipped on Tuesday for receipt on Wednesday or Thursday. As a biologic product that′s shipped at room temperature the cells must be processed immediately upon receipt.

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 knockout of the BCRP gene eliminates the reliance on chemical inhibitors to determine if a compound is an MDR1 substrate
  • The 24 well Transwell format enables the BCRP 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

Storage Class Code

13 - Non Combustible Solids

WGK

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
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
X Wu et al.
Pharmaceutical research, 17(2), 209-215 (2000-04-06)
The purpose of this study was to elucidate the mechanisms by which an HMG-CoA reductase inhibitor, atorvastatin (an organic acid with a pKa of 4.46), was transported in the secretory and absorptive directions across Caco-2 cell monolayers. Caco-2 cells were
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
Kathleen E Sampson et al.
Drug metabolism and disposition: the biological fate of chemicals, 43(2), 199-207 (2014-11-13)
Membrane transporters P-glycoprotein [P-gp; multidrug resistance 1 (MDR1)], multidrug resistance-associated protein (MRP) 2, and breast cancer resistance protein (BCRP) affect drug absorption and disposition and can also mediate drug-drug interactions leading to safety/toxicity concerns in the clinic. Challenges arise with
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Articles

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.

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.

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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