Elacridar hydrochloride

Name: Elacridar hydrochloride
Brand: Tocris Bioscience
SKU: 4646
Rating: 5 (1 reviews)

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

(1)

Citations (7)

COA / SDS

P-gp and BCRP inhibitor

Key Product Details

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)
Molecular Weight:	600.1

View Full Technical Details for Elacridar hydrochloride

Technical Data
Citations / Reviews (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
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Elacridar hydrochloride

	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 600.1.

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

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Reconstitution Calculator

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References for Elacridar hydrochloride

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