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.

Product Specifications

Molecular Weight

600.10

Formula

C₃₄H₃₃N₃O₅.HCl

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

CAS Number

143851-98-3

PubChem ID

170320

InChI Key

IQOJZZHRYSSFJM-UHFFFAOYSA-N

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.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	12	20

Preparing Stock Solutions for Elacridar hydrochloride

The following data is based on the product molecular weight 600.10

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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

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Background References

References are publications that support the biological activity of the product.

Myer 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. 1999 PMID: 9864431
Durmus 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. 2012 PMID: 23020847
Hyafil In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 1993 PMID: 8402633

Elacridar hydrochloride

Tocris Bioscience, part of Bio-Techne | Catalog # 4646

Key Product Details

Description

Alternative Names

View all Multidrug Transporter Inhibitors »

Product Description