Elacridar hydrochloride
Chemical Name: N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide hydrochloride
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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Pro-inflammatory human Th17 cells selectively express P-glycoprotein and are refractory to glucocorticoids.
Ramesh R, Kozhaya L, McKevitt K, Djuretic I, Carlson T, Quintero M, McCauley J, Abreu M, Unutmaz D, Sundrud M
J Exp Med, 2014;211(1):89-104. -
In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative.
Hyafil et al.
Cancer Res., 1993;53:4595 -
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.
Myer et al.
Oncol Rep., 1999;6:217
Product Datasheets
Citations for Elacridar hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Elacridar hydrochloride include:
4 Citations: Showing 1 - 4
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Lower Tubulin Expression in Glioblastoma Stem Cells Attenuates Efficacy of Microtubule-Targeting Agents.
Authors: Terrance G Et al.
ACS Pharmacol Transl Sci 2019;2:402-413
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Systemic Administration of Glibenclamide Fails to Achieve Therapeutic Levels in the Brain and Cerebrospinal Fluid of Rodents.
Authors: Lahmann Et al.
PLoS One 2015;10:e0134476
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Pro-inflammatory human Th17 cells selectively express P-glycoprotein and are refractory to glucocorticoids.
Authors: Ramesh Et al.
J Exp Med 2014;211:89
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Inhibiting drug efflux transporters improves efficacy of ALS therapeutics.
Authors: Jablonski Et al.
Ann Clin Transl Neurol 2014;1:996
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