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Biological Activity for Elacridar hydrochloride
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.
Technical Data for Elacridar hydrochloride
|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.
Solubility Data for Elacridar hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Elacridar hydrochloride
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|
Product Datasheets for Elacridar hydrochloride
References for Elacridar hydrochloride
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
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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
3 Citations for Elacridar hydrochloride
Citations are publications that use Tocris products. Selected citations for Elacridar hydrochloride include:
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
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
Jablonski et al (2014) Inhibiting drug efflux transporters improves efficacy of ALS therapeutics. Ann Clin Transl Neurol 1 996 PMID: 25574474
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Reviews for Elacridar hydrochloride
Average Rating: 5 (Based on 1 Review.)
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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.
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