Elacridar hydrochloride

Pricing Availability   Qty
Description: P-gp and BCRP inhibitor
Alternative Names: GF 120918
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% (HPLC)
Citations (4)
Reviews (1)
Literature (1)

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data for Elacridar hydrochloride

M. Wt 600.1
Formula C34H33N3O5.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 143851-98-3
PubChem ID 170320
Smiles O=C1C3=C(C(C(NC4=CC=C(CCN5CC(C=C(OC)C(OC)=C6)=C6CC5)C=C4)=O)=CC=C3)NC2=C1C=CC=C2OC.Cl

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
DMSO 12 20

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Elacridar hydrochloride

Certificate of Analysis / Product Datasheet
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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

If you know of a relevant reference for Elacridar hydrochloride, please let us know.

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4 Citations for Elacridar hydrochloride

Citations are publications that use Tocris products. Selected citations for Elacridar hydrochloride include:

Terrance G et al (2019) Lower Tubulin Expression in Glioblastoma Stem Cells Attenuates Efficacy of Microtubule-Targeting Agents. ACS Pharmacol Transl Sci 2 402-413 PMID: 32259073

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.

Reviews for Elacridar hydrochloride

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1uM of elacridar is used to block the p glycoprotein.
By Shashirekha Shamamandri Markandaiah on 10/29/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Endothelial cell, Astrocytes

Elacridar is used as P glycoprotein transporter blocker to enhance drug penetration in iPsc derived endothelial cell co cultured with ALS astrocytes.

Literature in this Area

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