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Elacridar hydrochloride is a P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) inhibitor. Elacridar hydrochloride blocks P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs doxorubicin (Cat. No. 2252) and vincristine (Cat. No. 1257) in CHRC5 cells. Orally active.
Sold for research purposes under agreement from GlaxoSmithKline.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 600.1. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||8.33 mL||41.66 mL||83.32 mL|
|1 mM||1.67 mL||8.33 mL||16.66 mL|
|2 mM||0.83 mL||4.17 mL||8.33 mL|
|10 mM||0.17 mL||0.83 mL||1.67 mL|
References are publications that support the biological activity of the product.
Hyafil et al (1993) In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 53 4595 PMID: 8402633
Myer et al (1999) The chemosensitizing potential of GF120918 is independent of the magnitude of P-glycoprotein-mediated resistance to conventional chemotherapeutic agents in a small cell lung cancer line. Oncol Rep. 6 217 PMID: 9864431
Durmus et al (2012) Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. Mol.Pharm. 9 3236 PMID: 23020847
If you know of a relevant reference for Elacridar hydrochloride, please let us know.
Keywords: Elacridar hydrochloride, Elacridar hydrochloride supplier, GF120918, P-glycoprotein, P-gp, inhibitors, inhibits, multidrug, resistance, MDR, BCRP, ABCG2, ABCB1, GF, 120918, Multidrug, Transporters, 4646, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Elacridar hydrochloride include:
Ramesh et al (2014) Pro-inflammatory human Th17 cells selectively express P-glycoprotein and are refractory to glucocorticoids. J Exp Med 211 89 PMID: 24395888
Lahmann et al (2015) Systemic Administration of Glibenclamide Fails to Achieve Therapeutic Levels in the Brain and Cerebrospinal Fluid of Rodents. PLoS One 10 e0134476 PMID: 26225433
Jablonski et al (2014) Inhibiting drug efflux transporters improves efficacy of ALS therapeutics. Ann Clin Transl Neurol 1 996 PMID: 25574474
Do you know of a great paper that uses Elacridar hydrochloride from Tocris? Please let us know.
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Elacridar is used as P glycoprotein transporter blocker to enhance drug penetration in iPsc derived endothelial cell co cultured with ALS astrocytes.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.